fedratinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5347	936091-26-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: fedratinib fedratinib hydrochloride SAR302503 SAR-302503 TG101348 TG-101348 FEDR inrebic	Fedratinib is an oral kinase inhibitor with activity against wild type and mutationally activated Janus Associated Kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3). Fedratinib is a JAK2-selective inhibitor with higher inhibitory activity for JAK2 over family members JAK1, JAK3 and TYK2. Abnormal activation of JAK2 is associated with myeloproliferative neoplasms (MPNs), including myelofibrosis and polycythemia vera. Molecular weight: 524.68 Formula: C27H36N6O3S CLOGP: 6.25 LIPINSKI: 2 HAC: 9 HDO: 3 TPSA: 108.48 ALOGS: -4.74 ROTB: 10 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

fedratinib
fedratinib hydrochloride
SAR302503
SAR-302503
TG101348
TG-101348
FEDR
inrebic

Fedratinib is an oral kinase inhibitor with activity against wild type and mutationally activated Janus Associated Kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3). Fedratinib is a JAK2-selective inhibitor with higher inhibitory activity for JAK2 over family members JAK1, JAK3 and TYK2. Abnormal activation of JAK2 is associated with myeloproliferative neoplasms (MPNs), including myelofibrosis and polycythemia vera.

Molecular weight: 524.68
Formula: C27H36N6O3S
CLOGP: 6.25
LIPINSKI: 2
HAC: 9
HDO: 3
TPSA: 108.48
ALOGS: -4.74
ROTB: 10

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.40	g	O

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Feb. 8, 2021	EMA	CELGENE EUROPE BV
Aug. 16, 2019	FDA	IMPACT

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Vitamin B1 decreased	103.24	41.87	13	503	199	63488307
Vitamin B1 deficiency	63.88	41.87	9	507	331	63488175
Diarrhoea	56.59	41.87	46	470	715320	62773186

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Vitamin B1 decreased	130.82	43.87	18	469	320	34956124
Vitamin B1 deficiency	122.51	43.87	17	470	322	34956122
Death	60.83	43.87	47	440	398002	34558442

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Vitamin B1 decreased	248.43	39.24	31	519	532	79743306
Vitamin B1 deficiency	172.34	39.24	23	527	675	79743163
Death	88.69	39.24	52	498	566462	79177376

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EJ02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Janus-associated kinase (JAK) inhibitors

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Myelofibrosis	indication	52967002	DOID:4971
Primary myelofibrosis	indication	307651005
Post-polycythaemia vera myelofibrosis	indication	871540009
Post-essential thrombocythaemia myelofibrosis	indication	871541008

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.42	acidic
pKa2	8.9	Basic
pKa3	5.69	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 100MG BASE	INREBIC	IMPACT	N212327	Aug. 16, 2019	RX	CAPSULE	ORAL	8138199	June 30, 2028	TREATMENT OF ADULT PATIENTS WITH INTERMEDIATE-2 OR HIGH-RISK PRIMARY OR SECONDARY MYELOFIBROSIS
EQ 100MG BASE	INREBIC	IMPACT	N212327	Aug. 16, 2019	RX	CAPSULE	ORAL	10391094	June 4, 2032	TREATMENT OF ADULT PATIENTS WITH INTERMEDIATE-2 OR HIGH-RISK PRIMARY OR SECONDARY MYELOFIBROSIS
EQ 100MG BASE	INREBIC	IMPACT	N212327	Aug. 16, 2019	RX	CAPSULE	ORAL	11400092	Sept. 24, 2039	TREATING ADULT PATIENTS WITH INTERMEDIATE-2 OR HIGH-RISK PRIMARY OR SECONDARY MYELOFIBROSIS, MONITORING THIAMINE LEVELS AND ADMINISTERING THIAMINE OR A THIAMINE EQUIVALENT

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 100MG BASE	INREBIC	IMPACT	N212327	Aug. 16, 2019	RX	CAPSULE	ORAL	Aug. 16, 2024	NEW CHEMICAL ENTITY
EQ 100MG BASE	INREBIC	IMPACT	N212327	Aug. 16, 2019	RX	CAPSULE	ORAL	Aug. 16, 2026	INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH INTERMEDIATE-2 OR HIGH-RISK PRIMARY OR SECONDARY (POST-POLYCYTHEMIA VERA OR POST-ESSENTIAL THROMBOCYTHEMIA) MYELOFIBROSIS (MF)

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN	INHIBITOR	IC50	7.82	SCIENTIFIC LITERATURE	DRUG LABEL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN	INHIBITOR	IC50	8.52	SCIENTIFIC LITERATURE	DRUG LABEL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		Kd	7.40	CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN		Kd	7.34	CHEMBL
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		Kd	6.24	CHEMBL
Breakpoint cluster region protein	Kinase	P11274	BCR_HUMAN		Kd	5.76	CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN		Kd	7.12	CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	7.14	CHEMBL
Tyrosine-protein kinase Yes	Kinase	P07947	YES_HUMAN		Kd	6.92	CHEMBL
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		Kd	7.42	CHEMBL
Ephrin type-A receptor 2	Kinase	P29317	EPHA2_HUMAN		Kd	5.36	CHEMBL
Serine/threonine-protein kinase B-raf	Kinase	P15056	BRAF_HUMAN		Kd	5.03	CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		IC50	7.32	CHEMBL
Vascular endothelial growth factor receptor 1	Kinase	P17948	VGFR1_HUMAN		Kd	5.37	CHEMBL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN		Kd	5.28	CHEMBL
Vascular endothelial growth factor receptor 3	Kinase	P35916	VGFR3_HUMAN		Kd	5.70	CHEMBL
Macrophage colony-stimulating factor 1 receptor	Kinase	P07333	CSF1R_HUMAN		Kd	6.21	CHEMBL
Platelet-derived growth factor receptor alpha	Kinase	P16234	PGFRA_HUMAN		Kd	5.57	CHEMBL
Ribosomal protein S6 kinase alpha-3	Kinase	P51812	KS6A3_HUMAN		Kd	5.09	CHEMBL
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform	Kinase	P15735	PHKG2_HUMAN		Kd	5.80	CHEMBL
Insulin-like growth factor 1 receptor	Kinase	P08069	IGF1R_HUMAN		Kd	5.66	CHEMBL
Myosin light chain kinase, smooth muscle	Kinase	Q15746	MYLK_HUMAN		Kd	6.28	CHEMBL
Insulin receptor	Kinase	P06213	INSR_HUMAN		Kd	6.07	CHEMBL
Death-associated protein kinase 3	Kinase	O43293	DAPK3_HUMAN		Kd	8.92	CHEMBL
Calcium/calmodulin-dependent protein kinase type 1	Kinase	Q14012	KCC1A_HUMAN		Kd	5.80	CHEMBL
Mitogen-activated protein kinase 8	Kinase	P45983	MK08_HUMAN		Kd	6.58	CHEMBL
Fibroblast growth factor receptor 3	Kinase	P22607	FGFR3_HUMAN		Kd	6.44	CHEMBL
Rho-associated protein kinase 1	Kinase	Q13464	ROCK1_HUMAN		Kd	5.68	CHEMBL
Focal adhesion kinase 1	Kinase	Q05397	FAK1_HUMAN		Kd	7.38	CHEMBL
Tyrosine-protein kinase HCK	Kinase	P08631	HCK_HUMAN		Kd	5.68	CHEMBL
Serine/threonine-protein kinase PLK1	Kinase	P53350	PLK1_HUMAN		Kd	6.55	CHEMBL
Receptor tyrosine-protein kinase erbB-4	Kinase	Q15303	ERBB4_HUMAN		Kd	5.70	CHEMBL
Mitogen-activated protein kinase 10	Kinase	P53779	MK10_HUMAN		Kd	6.70	CHEMBL
Death-associated protein kinase 2	Kinase	Q9UIK4	DAPK2_HUMAN		Kd	7.54	CHEMBL
High affinity nerve growth factor receptor	Kinase	P04629	NTRK1_HUMAN		Kd	6.08	CHEMBL
Rho-associated protein kinase 2	Kinase	O75116	ROCK2_HUMAN		Kd	5.66	CHEMBL
Tyrosine-protein kinase SYK	Kinase	P43405	KSYK_HUMAN		Kd	5.57	CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta	Kinase	Q13557	KCC2D_HUMAN		Kd	6.23	CHEMBL
Myosin light chain kinase 2, skeletal/cardiac muscle	Kinase	Q9H1R3	MYLK2_HUMAN		Kd	5.52	CHEMBL
Tyrosine-protein kinase CSK	Kinase	P41240	CSK_HUMAN		Kd	5.23	CHEMBL
Angiopoietin-1 receptor	Kinase	Q02763	TIE2_HUMAN		Kd	5.72	CHEMBL
Ephrin type-A receptor 8	Kinase	P29322	EPHA8_HUMAN		Kd	5.11	CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit gamma	Kinase	Q13555	KCC2G_HUMAN		Kd	6.27	CHEMBL
AP2-associated protein kinase 1	Kinase	Q2M2I8	AAK1_HUMAN		Kd	7.46	CHEMBL
Serine/threonine-protein kinase MARK2	Kinase	Q7KZI7	MARK2_HUMAN		Kd	5.51	CHEMBL
Hepatocyte growth factor receptor	Kinase	P08581	MET_HUMAN		Kd	5.36	CHEMBL
Tyrosine-protein kinase Lyn	Kinase	P07948	LYN_HUMAN		Kd	6.30	CHEMBL
Cytoplasmic tyrosine-protein kinase BMX	Kinase	P51813	BMX_HUMAN		Kd	5.92	CHEMBL
Serine/threonine-protein kinase Nek2	Kinase	P51955	NEK2_HUMAN		Kd	5.77	CHEMBL
LIM domain kinase 1	Kinase	P53667	LIMK1_HUMAN		Kd	6.03	CHEMBL
Ribosomal protein S6 kinase alpha-2	Kinase	Q15349	KS6A2_HUMAN		Kd	5.64	CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-1	Kinase	Q13131	AAPK1_HUMAN		Kd	5.62	CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit beta	Kinase	Q13554	KCC2B_HUMAN		Kd	5.17	CHEMBL
Fibroblast growth factor receptor 1	Kinase	P11362	FGFR1_HUMAN		Kd	6.55	CHEMBL
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform	Kinase	Q16816	PHKG1_HUMAN		Kd	6.48	CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit alpha	Kinase	Q9UQM7	KCC2A_HUMAN		Kd	6.52	CHEMBL
Serine/threonine-protein kinase 17B	Kinase	O94768	ST17B_HUMAN		Kd	7.35	CHEMBL
Serine/threonine-protein kinase 10	Kinase	O94804	STK10_HUMAN		Kd	5.54	CHEMBL
Tyrosine-protein kinase Fer	Kinase	P16591	FER_HUMAN		Kd	5.96	CHEMBL
Protein kinase C epsilon type	Kinase	Q02156	KPCE_HUMAN		Kd	5.09	CHEMBL
Serine/threonine-protein kinase PLK4	Kinase	O00444	PLK4_HUMAN		Kd	7.02	CHEMBL
Aurora kinase C	Kinase	Q9UQB9	AURKC_HUMAN		Kd	6.46	CHEMBL
Serine/threonine-protein kinase 16	Kinase	O75716	STK16_HUMAN		Kd	8.18	CHEMBL
Dual specificity protein kinase TTK	Kinase	P33981	TTK_HUMAN		Kd	6.35	CHEMBL
Abelson tyrosine-protein kinase 2	Kinase	P42684	ABL2_HUMAN		Kd	6.24	CHEMBL
Ephrin type-A receptor 4	Kinase	P54764	EPHA4_HUMAN		Kd	5.40	CHEMBL
Fibroblast growth factor receptor 2	Kinase	P21802	FGFR2_HUMAN		Kd	6.33	CHEMBL
Serine/threonine-protein kinase N1	Kinase	Q16512	PKN1_HUMAN		Kd	5.96	CHEMBL
Serine/threonine-protein kinase 17A	Kinase	Q9UEE5	ST17A_HUMAN		Kd	6.21	CHEMBL
Ephrin type-A receptor 6	Kinase	Q9UF33	EPHA6_HUMAN		Kd	5.41	CHEMBL
Tyrosine-protein kinase Fgr	Kinase	P09769	FGR_HUMAN		Kd	7.09	CHEMBL
Aurora kinase A	Kinase	O14965	AURKA_HUMAN		Kd	5.36	CHEMBL
ALK tyrosine kinase receptor	Kinase	Q9UM73	ALK_HUMAN		Kd	6.19	CHEMBL
Serine/threonine-protein kinase 36	Kinase	Q9NRP7	STK36_HUMAN		Kd	6.06	CHEMBL
Ephrin type-A receptor 3	Kinase	P29320	EPHA3_HUMAN		Kd	5.15	CHEMBL
BMP-2-inducible protein kinase	Kinase	Q9NSY1	BMP2K_HUMAN		Kd	7.50	CHEMBL
Tyrosine-protein kinase FRK	Kinase	P42685	FRK_HUMAN		Kd	6.70	CHEMBL
Dual specificity protein kinase CLK1	Kinase	P49759	CLK1_HUMAN		Kd	5.60	CHEMBL
Dual specificity protein kinase CLK2	Kinase	P49760	CLK2_HUMAN		Kd	5.64	CHEMBL
Mitogen-activated protein kinase kinase kinase 4	Kinase	Q9Y6R4	M3K4_HUMAN		Kd	5.39	CHEMBL
Cyclin-G-associated kinase	Kinase	O14976	GAK_HUMAN		Kd	8.96	CHEMBL
Receptor-interacting serine/threonine-protein kinase 2	Kinase	O43353	RIPK2_HUMAN		Kd	5.21	CHEMBL
Ephrin type-B receptor 1	Kinase	P54762	EPHB1_HUMAN		Kd	5.77	CHEMBL
Calcium/calmodulin-dependent protein kinase type 1D	Kinase	Q8IU85	KCC1D_HUMAN		Kd	6.34	CHEMBL
Cyclin-dependent kinase 16	Kinase	Q00536	CDK16_HUMAN		Kd	5.51	CHEMBL
Activated CDC42 kinase 1	Kinase	Q07912	ACK1_HUMAN		Kd	7.19	CHEMBL
Ephrin type-A receptor 7	Kinase	Q15375	EPHA7_HUMAN		Kd	5.19	CHEMBL
Ribosomal protein S6 kinase alpha-5	Kinase	O75582	KS6A5_HUMAN		Kd	5.66	CHEMBL
STE20-like serine/threonine-protein kinase	Kinase	Q9H2G2	SLK_HUMAN		Kd	6.17	CHEMBL
Dual specificity protein kinase CLK4	Kinase	Q9HAZ1	CLK4_HUMAN		Kd	5.70	CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 2	Kinase	Q9HBH9	MKNK2_HUMAN		Kd	6.42	CHEMBL
Mitogen-activated protein kinase 9	Kinase	P45984	MK09_HUMAN		Kd	6.62	CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2	Kinase	Q96RR4	KKCC2_HUMAN		Kd	5.40	CHEMBL
MAP/microtubule affinity-regulating kinase 3	Kinase	P27448	MARK3_HUMAN		Kd	6.52	CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 1	Kinase	Q8N5S9	KKCC1_HUMAN		Kd	5.75	CHEMBL
Calcium/calmodulin-dependent protein kinase type 1G	Kinase	Q96NX5	KCC1G_HUMAN		Kd	5.50	CHEMBL
Epithelial discoidin domain-containing receptor 1	Kinase	Q08345	DDR1_HUMAN		Kd	5.72	CHEMBL
Ephrin type-B receptor 4	Kinase	P54760	EPHB4_HUMAN		Kd	5.68	CHEMBL
Testis-specific serine/threonine-protein kinase 1	Kinase	Q9BXA7	TSSK1_HUMAN		Kd	5.89	CHEMBL
Activin receptor type-1B	Kinase	P36896	ACV1B_HUMAN		Kd	5.17	CHEMBL
Serine/threonine-protein kinase receptor R3	Kinase	P37023	ACVL1_HUMAN		Kd	5.62	CHEMBL
Activin receptor type-1	Kinase	Q04771	ACVR1_HUMAN		Kd	6.82	CHEMBL
Cyclin-dependent kinase 15	Kinase	Q96Q40	CDK15_HUMAN		Kd	5.07	CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit beta	Kinase	O14920	IKKB_HUMAN		Kd	6.44	CHEMBL
TGF-beta receptor type-2	Kinase	P37173	TGFR2_HUMAN		Kd	5.96	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 1	Kinase	Q02750	MP2K1_HUMAN		Kd	5.29	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 2	Kinase	P36507	MP2K2_HUMAN		Kd	5.51	CHEMBL
Tyrosine-protein kinase ITK/TSK	Kinase	Q08881	ITK_HUMAN		Kd	6.31	CHEMBL
Tyrosine-protein kinase ZAP-70	Kinase	P43403	ZAP70_HUMAN		Kd	5.42	CHEMBL
Cyclin-dependent kinase 9	Kinase	P50750	CDK9_HUMAN		Kd	5.06	CHEMBL
Protein-tyrosine kinase 6	Kinase	Q13882	PTK6_HUMAN		Kd	5.92	CHEMBL
Tyrosine-protein kinase BTK	Kinase	Q06187	BTK_HUMAN		Kd	6.07	CHEMBL
Tyrosine-protein kinase receptor UFO	Kinase	P30530	UFO_HUMAN		Kd	6.80	CHEMBL
BDNF/NT-3 growth factors receptor	Kinase	Q16620	NTRK2_HUMAN		Kd	5.51	CHEMBL
Ephrin type-B receptor 2	Kinase	P29323	EPHB2_HUMAN		Kd	5.41	CHEMBL
Cyclin-dependent kinase 7	Kinase	P50613	CDK7_HUMAN		Kd	6.92	CHEMBL
Ribosomal protein S6 kinase beta-1	Kinase	P23443	KS6B1_HUMAN		Kd	5.70	CHEMBL
Serine/threonine-protein kinase DCLK3	Kinase	Q9C098	DCLK3_HUMAN		Kd	7.89	CHEMBL
Ribosomal protein S6 kinase alpha-6	Kinase	Q9UK32	KS6A6_HUMAN		Kd	6.44	CHEMBL
NUAK family SNF1-like kinase 2	Kinase	Q9H093	NUAK2_HUMAN		Kd	7.31	CHEMBL
Non-receptor tyrosine-protein kinase TNK1	Kinase	Q13470	TNK1_HUMAN		Kd	6.44	CHEMBL
Serine/threonine-protein kinase Chk1	Kinase	O14757	CHK1_HUMAN		Kd	5.42	CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform	Kinase	P42336	PK3CA_HUMAN		Kd	5.41	CHEMBL
Cyclin-dependent kinase 17	Kinase	Q00537	CDK17_HUMAN		Kd	6.46	CHEMBL
Cyclin-dependent kinase 18	Kinase	Q07002	CDK18_HUMAN		Kd	5.57	CHEMBL
Cyclin-dependent kinase 14	Kinase	O94921	CDK14_HUMAN		Kd	5.58	CHEMBL
Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha	Kinase	Q99755	PI51A_HUMAN		Kd	7.18	CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 beta	Kinase	P78356	PI42B_HUMAN		Kd	6.80	CHEMBL
Myosin light chain kinase family member 4	Kinase	Q86YV6	MYLK4_HUMAN		Kd	6.89	CHEMBL
Wee1-like protein kinase	Kinase	P30291	WEE1_HUMAN		Kd	6.41	CHEMBL
Serine/threonine-protein kinase 25	Kinase	O00506	STK25_HUMAN		Kd	5.14	CHEMBL
Mitogen-activated protein kinase kinase kinase MLT	Kinase	Q9NYL2	MLTK_HUMAN		Kd	6.19	CHEMBL
Protein-tyrosine kinase 2-beta	Kinase	Q14289	FAK2_HUMAN		Kd	6.66	CHEMBL
Serine/threonine-protein kinase RIO1	Kinase	Q9BRS2	RIOK1_HUMAN		Kd	7	CHEMBL
Tyrosine-protein kinase receptor Tie-1	Kinase	P35590	TIE1_HUMAN		Kd	6.16	CHEMBL
Serine/threonine-protein kinase tousled-like 1	Kinase	Q9UKI8	TLK1_HUMAN		Kd	5.89	CHEMBL
Serine/threonine-protein kinase tousled-like 2	Kinase	Q86UE8	TLK2_HUMAN		Kd	5.70	CHEMBL
NT-3 growth factor receptor	Kinase	Q16288	NTRK3_HUMAN		Kd	5.07	CHEMBL
Tyrosine-protein kinase TXK	Kinase	P42681	TXK_HUMAN		Kd	5.82	CHEMBL
Casein kinase II subunit alpha	Kinase	P68400	CSK21_HUMAN		Kd	6.04	CHEMBL
Casein kinase II subunit alpha'	Kinase	P19784	CSK22_HUMAN		Kd	6.92	CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1B	Kinase	Q9Y463	DYR1B_HUMAN		Kd	5.02	CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon	Kinase	Q14164	IKKE_HUMAN		Kd	6.44	CHEMBL
LIM domain kinase 2	Kinase	P53671	LIMK2_HUMAN		Kd	5.10	CHEMBL
Serine/threonine-protein kinase STK11	Kinase	Q15831	STK11_HUMAN		Kd	6.51	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 3	Kinase	P46734	MP2K3_HUMAN		Kd	5.46	CHEMBL
Maternal embryonic leucine zipper kinase	Kinase	Q14680	MELK_HUMAN		Kd	5.58	CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 1	Kinase	Q9BUB5	MKNK1_HUMAN		Kd	5.14	CHEMBL
Serine/threonine-protein kinase 26	Kinase	Q9P289	STK26_HUMAN		Kd	5.12	CHEMBL
Serine/threonine-protein kinase Nek7	Kinase	Q8TDX7	NEK7_HUMAN		Kd	6.80	CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 4	Kinase	Q9P2K8	E2AK4_HUMAN		Kd	7	CHEMBL
Insulin receptor-related protein	Kinase	P14616	INSRR_HUMAN		Kd	5.80	CHEMBL
Interleukin-1 receptor-associated kinase 3	Kinase	Q9Y616	IRAK3_HUMAN		Kd	6.92	CHEMBL
Serine/threonine-protein kinase RIO3	Kinase	O14730	RIOK3_HUMAN		Kd	7.04	CHEMBL
Serine/threonine-protein kinase SIK2	Kinase	Q9H0K1	SIK2_HUMAN		Kd	7.01	CHEMBL
SRSF protein kinase 1	Kinase	Q96SB4	SRPK1_HUMAN		Kd	6.80	CHEMBL
SRSF protein kinase 2	Kinase	P78362	SRPK2_HUMAN		Kd	7	CHEMBL
Serine/threonine-protein kinase 33	Kinase	Q9BYT3	STK33_HUMAN		Kd	6.66	CHEMBL
Serine/threonine-protein kinase TNNI3K	Kinase	Q59H18	TNI3K_HUMAN		Kd	5.75	CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-2	Kinase	P54646	AAPK2_HUMAN		Kd	5.33	CHEMBL
Ankyrin repeat and protein kinase domain-containing protein 1	Kinase	Q8NFD2	ANKK1_HUMAN		Kd	5.37	CHEMBL
Discoidin domain-containing receptor 2	Kinase	Q16832	DDR2_HUMAN		Kd	6.02	CHEMBL
Myotonin-protein kinase	Kinase	Q09013	DMPK_HUMAN		Kd	6	CHEMBL
Chaperone activity of bc1 complex-like, mitochondrial	Kinase	Q8NI60	COQ8A_HUMAN		Kd	5.16	CHEMBL
Serine/threonine-protein kinase LATS2	Kinase	Q9NRM7	LATS2_HUMAN		Kd	5.10	CHEMBL
Leukocyte tyrosine kinase receptor	Kinase	P29376	LTK_HUMAN		Kd	5.20	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1	Kinase	Q92918	M4K1_HUMAN		Kd	5.89	CHEMBL
Serine/threonine-protein kinase PAK 6	Kinase	Q9NQU5	PAK6_HUMAN		Kd	5.16	CHEMBL
Serine/threonine-protein kinase PAK 7	Kinase	Q9P286	PAK5_HUMAN		Kd	5.92	CHEMBL
NUAK family SNF1-like kinase 1	Kinase	O60285	NUAK1_HUMAN		Kd	7.47	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3	Kinase	Q8IVH8	M4K3_HUMAN		Kd	5.75	CHEMBL
Aurora kinase B	Kinase	Q96GD4	AURKB_HUMAN		Kd	6.31	CHEMBL
Tyrosine-protein kinase Blk	Kinase	P51451	BLK_HUMAN		Kd	6.19	CHEMBL
Bone morphogenetic protein receptor type-2	Kinase	Q13873	BMPR2_HUMAN		Kd	5.54	CHEMBL
Serine/threonine-protein kinase MARK1	Kinase	Q9P0L2	MARK1_HUMAN		Kd	6.16	CHEMBL
MAP/microtubule affinity-regulating kinase 4	Kinase	Q96L34	MARK4_HUMAN		Kd	6.01	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 4	Kinase	P45985	MP2K4_HUMAN		Kd	5	CHEMBL
Tyrosine-protein kinase Mer	Kinase	Q12866	MERTK_HUMAN		Kd	6.09	CHEMBL
Mitogen-activated protein kinase kinase kinase 9	Kinase	P80192	M3K9_HUMAN		Kd	5.50	CHEMBL
Mitogen-activated protein kinase kinase kinase 10	Kinase	Q02779	M3K10_HUMAN		Kd	5.16	CHEMBL
Mitogen-activated protein kinase kinase kinase 11	Kinase	Q16584	M3K11_HUMAN		Kd	5.51	CHEMBL
Muscle, skeletal receptor tyrosine-protein kinase	Kinase	O15146	MUSK_HUMAN		Kd	6.10	CHEMBL
Citron Rho-interacting kinase	Kinase	O14578	CTRO_HUMAN		Kd	6.85	CHEMBL
Death-associated protein kinase 1	Kinase	P53355	DAPK1_HUMAN		Kd	7.80	CHEMBL
Serine/threonine-protein kinase DCLK1	Kinase	O15075	DCLK1_HUMAN		Kd	6.72	CHEMBL
Serine/threonine-protein kinase DCLK2	Kinase	Q8N568	DCLK2_HUMAN		Kd	6.06	CHEMBL
Serine/threonine-protein kinase Nek5	Kinase	Q6P3R8	NEK5_HUMAN		Kd	6.24	CHEMBL
Serine/threonine-protein kinase Nek9	Kinase	Q8TD19	NEK9_HUMAN		Kd	6.82	CHEMBL
Serine/threonine-protein kinase PAK 1	Kinase	Q13153	PAK1_HUMAN		Kd	5.51	CHEMBL
Serine/threonine-protein kinase PAK 2	Kinase	Q13177	PAK2_HUMAN		Kd	5.22	CHEMBL
Serine/threonine-protein kinase PAK 4	Kinase	O96013	PAK4_HUMAN		Kd	5.42	CHEMBL
AarF domain-containing protein kinase 4	Kinase	Q96D53	COQ8B_HUMAN		Kd	6.52	CHEMBL
Serine/threonine-protein kinase SIK1	Kinase	P57059	SIK1_HUMAN		Kd	7.41	CHEMBL
Tyrosine-protein kinase Srms	Kinase	Q9H3Y6	SRMS_HUMAN		Kd	5.30	CHEMBL
Dual specificity testis-specific protein kinase 1	Kinase	Q15569	TESK1_HUMAN		Kd	5.50	CHEMBL
Ephrin type-A receptor 1	Kinase	P21709	EPHA1_HUMAN		Kd	6.14	CHEMBL
Serine/threonine-protein kinase PLK3	Kinase	Q9H4B4	PLK3_HUMAN		Kd	5.80	CHEMBL
Mitogen-activated protein kinase 6	Kinase	Q16659	MK06_HUMAN		Kd	5.92	CHEMBL
Mitogen-activated protein kinase 7	Kinase	Q13164	MK07_HUMAN		Kd	7.18	CHEMBL
Mitogen-activated protein kinase 15	Kinase	Q8TD08	MK15_HUMAN		Kd	6.29	CHEMBL
Serine/threonine-protein kinase D3	Kinase	O94806	KPCD3_HUMAN		Kd	5.02	CHEMBL
cGMP-dependent protein kinase 2	Kinase	Q13237	KGP2_HUMAN		Kd	5.80	CHEMBL
Interferon-induced, double-stranded RNA-activated protein kinase	Kinase	P19525	E2AK2_HUMAN		Kd	5.96	CHEMBL
Receptor-interacting serine/threonine-protein kinase 1	Kinase	Q13546	RIPK1_HUMAN		Kd	5.28	CHEMBL
Tyrosine-protein kinase Fes/Fps	Kinase	P07332	FES_HUMAN		Kd	6.28	CHEMBL
Fibroblast growth factor receptor 4	Kinase	P22455	FGFR4_HUMAN		Kd	5.70	CHEMBL
Proto-oncogene tyrosine-protein kinase ROS	Kinase	P08922	ROS1_HUMAN		Kd	6.22	CHEMBL
Ribosomal protein S6 kinase alpha-1	Kinase	Q15418	KS6A1_HUMAN		Kd	6.38	CHEMBL
Ribosomal protein S6 kinase alpha-4	Kinase	O75676	KS6A4_HUMAN		Kd	6.85	CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform	Kinase	P48736	PK3CG_HUMAN		Kd	5.12	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2	Kinase	Q12851	M4K2_HUMAN		Kd	5.68	CHEMBL
Misshapen-like kinase 1	Kinase	Q8N4C8	MINK1_HUMAN		Kd	5.05	CHEMBL
Serine/threonine-protein kinase TBK1	Kinase	Q9UHD2	TBK1_HUMAN		Kd	7.04	CHEMBL
Interleukin-1 receptor-associated kinase 4	Kinase	Q9NWZ3	IRAK4_HUMAN		Kd	5.92	CHEMBL
Cyclin-dependent kinase 4	Kinase	P11802	CDK4_HUMAN		Kd	6.06	CHEMBL
Cyclin-dependent kinase-like 2	Kinase	Q92772	CDKL2_HUMAN		Kd	5.89	CHEMBL
Ephrin type-B receptor 6	Kinase	O15197	EPHB6_HUMAN		Kd	6.52	CHEMBL
Serine/threonine-protein kinase/endoribonuclease IRE1	Kinase	O75460	ERN1_HUMAN		Kd	5.92	CHEMBL
G protein-coupled receptor kinase 4	Kinase	P32298	GRK4_HUMAN		Kd	6.77	CHEMBL
G protein-coupled receptor kinase 7	Kinase	Q8WTQ7	GRK7_HUMAN		Kd	5.58	CHEMBL
Homeodomain-interacting protein kinase 2	Kinase	Q9H2X6	HIPK2_HUMAN		Kd	6	CHEMBL
Homeodomain-interacting protein kinase 3	Kinase	Q9H422	HIPK3_HUMAN		Kd	5.89	CHEMBL
Homeodomain-interacting protein kinase 4	Kinase	Q8NE63	HIPK4_HUMAN		Kd	6.66	CHEMBL
Serine/threonine-protein kinase ICK	Kinase	Q9UPZ9	ICK_HUMAN		Kd	5.72	CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit alpha	Kinase	O15111	IKKA_HUMAN		Kd	6.08	CHEMBL
Interleukin-1 receptor-associated kinase 1	Kinase	P51617	IRAK1_HUMAN		Kd	6.66	CHEMBL
Mitogen-activated protein kinase kinase kinase 13	Kinase	O43283	M3K13_HUMAN		Kd	6.23	CHEMBL
Mitogen-activated protein kinase kinase kinase 2	Kinase	Q9Y2U5	M3K2_HUMAN		Kd	6.24	CHEMBL
Mitogen-activated protein kinase kinase kinase 3	Kinase	Q99759	M3K3_HUMAN		Kd	5.89	CHEMBL
Serine/threonine-protein kinase 38	Kinase	Q15208	STK38_HUMAN		Kd	5.24	CHEMBL
Serine/threonine-protein kinase NIM1	Kinase	Q8IY84	NIM1_HUMAN		Kd	5.36	CHEMBL
Serine/threonine-protein kinase RIO2	Kinase	Q9BVS4	RIOK2_HUMAN		Kd	5.58	CHEMBL
SRSF protein kinase 3	Kinase	Q9UPE1	SRPK3_HUMAN		Kd	6.77	CHEMBL
STE20/SPS1-related proline-alanine-rich protein kinase	Kinase	Q9UEW8	STK39_HUMAN		Kd	5.80	CHEMBL
Mitogen-activated protein kinase kinase kinase 7	Kinase	O43318	M3K7_HUMAN		Kd	5.51	CHEMBL
Serine/threonine-protein kinase TAO1	Kinase	Q7L7X3	TAOK1_HUMAN		Kd	5.89	CHEMBL
Serine/threonine-protein kinase TAO3	Kinase	Q9H2K8	TAOK3_HUMAN		Kd	5.72	CHEMBL
Serine/threonine-protein kinase ULK1	Kinase	O75385	ULK1_HUMAN		Kd	6.57	CHEMBL
Serine/threonine-protein kinase ULK2	Kinase	Q8IYT8	ULK2_HUMAN		Kd	7.10	CHEMBL
Serine/threonine-protein kinase ULK3	Kinase	Q6PHR2	ULK3_HUMAN		Kd	6.54	CHEMBL
Mitogen-activated protein kinase kinase kinase 19	Kinase	Q56UN5	M3K19_HUMAN		Kd	7.72	CHEMBL
Homeodomain-interacting protein kinase 1	Kinase	Q86Z02	HIPK1_HUMAN		Kd	6.07	CHEMBL
Serine/threonine-protein kinase PLK2	Kinase	Q9NYY3	PLK2_HUMAN		Kd	5.62	CHEMBL
Receptor-interacting serine/threonine-protein kinase 4	Kinase	P57078	RIPK4_HUMAN		Kd	5.01	CHEMBL
Uncharacterized serine/threonine-protein kinase SBK3	Kinase	P0C264	SBK3_HUMAN		Kd	5.54	CHEMBL
Ribosyldihydronicotinamide dehydrogenase [quinone]	Enzyme	P16083	NQO2_HUMAN		Kd	5.37	CHEMBL
Megakaryocyte-associated tyrosine-protein kinase	Kinase	P42679	MATK_HUMAN		Kd	5.77	CHEMBL
Phosphatidylinositol 4-kinase beta	Kinase	Q9UBF8	PI4KB_HUMAN		Kd	5.77	CHEMBL
Serine/threonine-protein kinase SIK3	Kinase	Q9Y2K2	SIK3_HUMAN		Kd	5.72	CHEMBL
Wee1-like protein kinase 2	Kinase	P0C1S8	WEE2_HUMAN		Kd	5.22	CHEMBL
Bone morphogenetic protein receptor type-1B	Kinase	O00238	BMR1B_HUMAN		Kd	6.39	CHEMBL
Serine/threonine-protein kinase SBK1	Kinase	Q52WX2	SBK1_HUMAN		Kd	6.10	CHEMBL
Serine/threonine-protein kinase Nek3	Kinase	P51956	NEK3_HUMAN		Kd	6.19	CHEMBL
Peripheral plasma membrane protein CASK	Kinase	O14936	CSKP_HUMAN		Kd	5.55	CHEMBL
Serine/threonine-protein kinase PRP4 homolog	Kinase	Q13523	PRP4B_HUMAN		Kd	6.41	CHEMBL
Mitogen-activated protein kinase kinase kinase 12	Kinase	Q12852	M3K12_HUMAN		Kd	5.20	CHEMBL
Serine/threonine-protein kinase Sgk3	Kinase	Q96BR1	SGK3_HUMAN		Kd	5.60	CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 1	Kinase	Q9BQI3	E2AK1_HUMAN		Kd	6	CHEMBL
Serine/threonine-protein kinase TAO2	Kinase	Q9UL54	TAOK2_HUMAN		Kd	6.12	CHEMBL
SNF-related serine/threonine-protein kinase	Kinase	Q9NRH2	SNRK_HUMAN		Kd	6.64	CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma	Kinase	Q8TBX8	PI42C_HUMAN		Kd	5.39	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5	Kinase	Q13163	MP2K5_HUMAN		Kd	6.44	CHEMBL
Serine/threonine-protein kinase Nek11	Kinase	Q8NG66	NEK11_HUMAN		Kd	5.92	CHEMBL
Myosin light chain kinase 3	Kinase	Q32MK0	MYLK3_HUMAN		Kd	5.01	CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2	Kinase	Q5S007	LRRK2_HUMAN		Kd	6.06	CHEMBL
Dual serine/threonine and tyrosine protein kinase	Kinase	Q6XUX3	DUSTY_HUMAN		Kd	5.77	CHEMBL
Bromodomain-containing protein 4	Unclassified	O60885	BRD4_HUMAN		Kd	6.79	CHEMBL
Serine/threonine-protein kinase Nek6	Kinase	Q9HC98	NEK6_HUMAN		Kd	6.92	CHEMBL
cGMP-dependent protein kinase 1	Kinase	Q13976	KGP1_HUMAN		Kd	5.42	CHEMBL
Serine/threonine-protein kinase Nek4	Kinase	P51957	NEK4_HUMAN		Kd	5.80	CHEMBL
Bromodomain testis-specific protein	Unclassified	Q58F21	BRDT_HUMAN		IC50	6.47	CHEMBL
Serine/threonine-protein kinase Nek1	Kinase	Q96PY6	NEK1_HUMAN		Kd	5.47	CHEMBL
Uncharacterized protein FLJ45252	Unclassified	Q6ZSR9	YJ005_HUMAN		Kd	6.56	CHEMBL
Uncharacterized aarF domain-containing protein kinase 1	Kinase	Q86TW2	ADCK1_HUMAN		Kd	6.64	CHEMBL
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN	INHIBITOR	IC50	5.99	SCIENTIFIC LITERATURE
Tyrosine-protein kinase JAK1	Kinase	P23458	JAK1_HUMAN	INHIBITOR	IC50	6.97	SCIENTIFIC LITERATURE
Non-receptor tyrosine-protein kinase TYK2	Kinase	P29597	TYK2_HUMAN	INHIBITOR	IC50	6.39	SCIENTIFIC LITERATURE
Cyclin-dependent kinase-like 5	Kinase	O76039	CDKL5_HUMAN		Kd	5.14	CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN		Kd	7.35	CHEMBL
Calcium-dependent protein kinase 1	Kinase		CDPK1_PLAF7		Kd	5.92	CHEMBL
Serine/threonine-protein kinase PknB	Kinase		PKNB_MYCTU		Kd	7	CHEMBL

External reference:

ID	Source
6L1XP550I6	UNII
1374744-69-0	SECONDARY_CAS_RN
C3886623	UMLSCUI
2TA	PDB_CHEM_ID
CHEMBL1287853	ChEMBL_ID
16722836	PUBCHEM_CID
DB12500	DRUGBANK_ID
CHEMBL4297216	ChEMBL_ID
D10630	KEGG_DRUG
9707	INN_ID
5716	IUPHAR_LIGAND_ID
018090	NDDF
789359000	SNOMEDCT_US
789368003	SNOMEDCT_US
895592002	SNOMEDCT_US
4038661	VANDF
2197490	RXNORM
321679	MMSL
d09354	MMSL
C528327	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Inrebic	HUMAN PRESCRIPTION DRUG LABEL	1	59572-720	CAPSULE	100 mg	ORAL	NDA	31 sections
Inrebic	HUMAN PRESCRIPTION DRUG LABEL	1	59572-720	CAPSULE	100 mg	ORAL	NDA	31 sections
Inrebic	HUMAN PRESCRIPTION DRUG LABEL	1	59572-720	CAPSULE	100 mg	ORAL	NDA	31 sections