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

Stem definition	Drug id	CAS RN
	5231	120685-11-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: midostaurin CGP 41251 PKC 412 rydapt	Midostaurin is a small molecule that inhibits multiple receptor tyrosine kinases. In vitro biochemical or cellular assays have shown that midostaurin or its major human active metabolites CGP62221 and CGP52421 inhibit the activity of wild type FLT3, FLT3 mutant kinases (ITD and TKD), KIT (wild type and D816V mutant), PDGFR-alfa/beta, VEGFR2, as well as members of the serine/threonine kinase PKC (protein kinase C) family. Midostaurin demonstrated the ability to inhibit FLT3 receptor signaling and cell proliferation, and it induced apoptosis in leukemic cells expressing ITD and TKD mutant FLT3 receptors or overexpressing wild type FLT3 and PDGF receptors. Midostaurin also demonstrated the ability to inhibit KIT signaling, cell proliferation and histamine release and induce apoptosis in mast cells. Molecular weight: 570.65 Formula: C35H30N4O4 CLOGP: 5.53 LIPINSKI: 2 HAC: 8 HDO: 1 TPSA: 77.73 ALOGS: -4.56 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

midostaurin
CGP 41251
PKC 412
rydapt

Midostaurin is a small molecule that inhibits multiple receptor tyrosine kinases. In vitro biochemical or cellular assays have shown that midostaurin or its major human active metabolites CGP62221 and CGP52421 inhibit the activity of wild type FLT3, FLT3 mutant kinases (ITD and TKD), KIT (wild type and D816V mutant), PDGFR-alfa/beta, VEGFR2, as well as members of the serine/threonine kinase PKC (protein kinase C) family. Midostaurin demonstrated the ability to inhibit FLT3 receptor signaling and cell proliferation, and it induced apoptosis in leukemic cells expressing ITD and TKD mutant FLT3 receptors or overexpressing wild type FLT3 and PDGF receptors. Midostaurin also demonstrated the ability to inhibit KIT signaling, cell proliferation and histamine release and induce apoptosis in mast cells.

Molecular weight: 570.65
Formula: C35H30N4O4
CLOGP: 5.53
LIPINSKI: 2
HAC: 8
HDO: 1
TPSA: 77.73
ALOGS: -4.56
ROTB: 3

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.10	g	O

ADMET properties:

Property	Value	Reference
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
Sept. 18, 2017	EMA	Novartis Europharm Ltd
April 28, 2017	FDA	NOVARTIS PHARMS CORP

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
Acute myeloid leukaemia recurrent	178.25	34.17	33	2129	1590	63485270
Febrile neutropenia	152.39	34.17	76	2086	118373	63368487
Minimal residual disease	66.23	34.17	10	2152	134	63486726
Death	61.01	34.17	69	2093	374312	63112548
Thrombocytopenia	60.28	34.17	46	2116	151111	63335749
Neutropenic colitis	59.53	34.17	15	2147	3080	63483780
Cytopenia	47.41	34.17	17	2145	11584	63475276
Abdominal wall wound	47.00	34.17	7	2155	85	63486775
Sepsis	47.00	34.17	40	2122	153083	63333777
Myeloblast percentage decreased	43.39	34.17	6	2156	41	63486819
Iron overload	42.28	34.17	9	2153	882	63485978
Megacolon	35.43	34.17	9	2153	1906	63484954
Neutropenia	34.92	34.17	36	2126	174969	63311891

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
Acute myeloid leukaemia recurrent	262.17	34.02	54	2473	2116	34952288
Febrile neutropenia	135.86	34.02	97	2430	136752	34817652
Bone marrow failure	123.62	34.02	54	2473	29199	34925205
Skin toxicity	95.53	34.02	28	2499	4756	34949648
Pancytopenia	73.06	34.02	58	2469	95099	34859305
Tryptase increased	66.67	34.02	12	2515	225	34954179
Neutropenic colitis	60.99	34.02	18	2509	3126	34951278
Lymphadenopathy	58.05	34.02	32	2495	28431	34925973
Thrombocytopenia	46.98	34.02	57	2470	156190	34798214
Septic shock	43.04	34.02	38	2489	71796	34882608
Neutropenia	40.44	34.02	53	2474	156725	34797679
Pyrexia	34.82	34.02	75	2452	332938	34621466
Drug intolerance	34.64	34.02	31	2496	59539	34894865

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
Acute myeloid leukaemia recurrent	396.74	31.96	78	4151	3305	79736854
Febrile neutropenia	271.23	31.96	162	4067	230837	79509322
Bone marrow failure	141.51	31.96	64	4165	51043	79689116
Neutropenic colitis	131.71	31.96	35	4194	5672	79734487
Thrombocytopenia	103.24	31.96	96	4133	265163	79474996
Pancytopenia	101.64	31.96	78	4151	165667	79574492
Skin toxicity	88.76	31.96	28	4201	8286	79731873
Neutropenia	78.57	31.96	86	4143	287624	79452535
Tryptase increased	70.09	31.96	14	4215	639	79739520
Sepsis	67.45	31.96	77	4152	269351	79470808
Septic shock	62.79	31.96	52	4177	122749	79617410
Minimal residual disease	61.26	31.96	12	4217	495	79739664
Pyrexia	55.33	31.96	115	4114	678594	79061565
Cytopenia	45.42	31.96	22	4207	20361	79719798
Cytomegalovirus infection reactivation	44.78	31.96	17	4212	8699	79731460
Lymphadenopathy	43.81	31.96	30	4199	53217	79686942
Abdominal wall wound	43.10	31.96	7	4222	96	79740063
Death	41.46	31.96	92	4137	566422	79173737
Bacteraemia	40.77	31.96	24	4205	32800	79707359
Myeloblast percentage decreased	40.72	31.96	6	4223	41	79740118
Systemic mastocytosis	34.82	31.96	7	4222	330	79739829
Graft versus host disease	32.82	31.96	16	4213	15010	79725149
Pneumonia	32.28	31.96	92	4137	660154	79080005

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EX10	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors
FDA MoA	N0000020000	Receptor Tyrosine Kinase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:37700	protein kinase C inhibitors

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

Disease	Relation	SNOMED_ID	DOID
Acute myeloid leukemia, disease	indication	91861009
Mast cell leukemia	indication	110002002
Aggressive systemic mastocytosis	indication	716655008	DOID:4798

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.7	acidic

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
25MG	RYDAPT	NOVARTIS	N207997	April 28, 2017	RX	CAPSULE	ORAL	7973031	Oct. 9, 2028	TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED ACUTE MYELOID LEUKEMIA (AML) WHO ARE FLT3 MUTATION-POSITIVE, IN COMBINATION WITH STANDARD CYTARABINE AND DAUNORUBICIN INDUCTION AND CYTARABINE CONSOLIDATION CHEMOTHERAPY
25MG	RYDAPT	NOVARTIS	N207997	April 28, 2017	RX	CAPSULE	ORAL	8575146	Dec. 2, 2030	TREATMENT OF ADULT PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), OR MAST CELL LEUKEMIA (MCL)

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
25MG	RYDAPT	NOVARTIS	N207997	April 28, 2017	RX	CAPSULE	ORAL	April 28, 2024	TREATMENT OF ADULT PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), OR MAST CELL LEUKEMIA (MCL)
25MG	RYDAPT	NOVARTIS	N207997	April 28, 2017	RX	CAPSULE	ORAL	April 28, 2024	TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED ACUTE MYELOID LEUKEMIA (AML) THAT IS FLT3 MUTATION-POSITIVE AS DETECTED BY AN FDA APPROVED TEST, IN COMBINATION WITH STANDARD CYTARABINE AND DAUNORUBICIN INDUCTION AND CYTARABINE CONSOLIDATION

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	Kd	7.96	IUPHAR	DRUG LABEL
Serine/threonine-protein kinase pim-1	Kinase	P11309	PIM1_HUMAN		Kd	6.25	CHEMBL
Ribosomal protein S6 kinase alpha-3	Kinase	P51812	KS6A3_HUMAN		Kd	6.13	CHEMBL
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN		Kd	7.92	CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN		Kd	6.96	CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		Kd	6.10	CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN		Kd	8.11	CHEMBL
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		Kd	8.06	CHEMBL
Aspartyl/asparaginyl beta-hydroxylase	Enzyme	Q12797	ASPH_HUMAN		IC50	5.22	CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN		Kd	5.92	CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	6.55	CHEMBL
Tyrosine-protein kinase Yes	Kinase	P07947	YES_HUMAN		Kd	6.02	CHEMBL
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		Kd	5.68	CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		Kd	7.70	CHEMBL
Vascular endothelial growth factor receptor 1	Kinase	P17948	VGFR1_HUMAN		Kd	6.35	CHEMBL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN		IC50	6.60	CHEMBL
Vascular endothelial growth factor receptor 3	Kinase	P35916	VGFR3_HUMAN		Kd	6.17	CHEMBL
Macrophage colony-stimulating factor 1 receptor	Kinase	P07333	CSF1R_HUMAN		IC50	6.85	CHEMBL
Platelet-derived growth factor receptor alpha	Kinase	P16234	PGFRA_HUMAN		Kd	6.75	CHEMBL
Myosin light chain kinase, smooth muscle	Kinase	Q15746	MYLK_HUMAN		Kd	6.66	CHEMBL
Death-associated protein kinase 3	Kinase	O43293	DAPK3_HUMAN		Kd	5.75	CHEMBL
Calcium/calmodulin-dependent protein kinase type 1	Kinase	Q14012	KCC1A_HUMAN		Kd	5.70	CHEMBL
Mitogen-activated protein kinase 8	Kinase	P45983	MK08_HUMAN		Kd	5.36	CHEMBL
Fibroblast growth factor receptor 3	Kinase	P22607	FGFR3_HUMAN		Kd	5.77	CHEMBL
Rho-associated protein kinase 1	Kinase	Q13464	ROCK1_HUMAN		Kd	5.11	CHEMBL
Tyrosine-protein kinase HCK	Kinase	P08631	HCK_HUMAN		Kd	6.14	CHEMBL
Tyrosine-protein kinase JAK1	Kinase	P23458	JAK1_HUMAN		Kd	6.17	CHEMBL
Receptor tyrosine-protein kinase erbB-4	Kinase	Q15303	ERBB4_HUMAN		Kd	5.51	CHEMBL
Mitogen-activated protein kinase 10	Kinase	P53779	MK10_HUMAN		Kd	5.44	CHEMBL
Death-associated protein kinase 2	Kinase	Q9UIK4	DAPK2_HUMAN		Kd	6.05	CHEMBL
High affinity nerve growth factor receptor	Kinase	P04629	NTRK1_HUMAN		Kd	6.42	CHEMBL
Protein kinase C delta type	Kinase	Q05655	KPCD_HUMAN		Kd	6.50	CHEMBL
cAMP-dependent protein kinase catalytic subunit beta	Kinase	P22694	KAPCB_HUMAN		Kd	6.62	CHEMBL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN		Kd	7.03	CHEMBL
Rho-associated protein kinase 2	Kinase	O75116	ROCK2_HUMAN		Kd	5.64	CHEMBL
Protein kinase C alpha type	Kinase	P17252	KPCA_HUMAN		Kd	6.14	CHEMBL
Tyrosine-protein kinase SYK	Kinase	P43405	KSYK_HUMAN		Kd	7.06	CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta	Kinase	Q13557	KCC2D_HUMAN		Kd	7.44	CHEMBL
Tyrosine-protein kinase CSK	Kinase	P41240	CSK_HUMAN		Kd	5.06	CHEMBL
Angiopoietin-1 receptor	Kinase	Q02763	TIE2_HUMAN		Kd	5.72	CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit gamma	Kinase	Q13555	KCC2G_HUMAN		Kd	6.85	CHEMBL
AP2-associated protein kinase 1	Kinase	Q2M2I8	AAK1_HUMAN		Kd	7.32	CHEMBL
Serine/threonine-protein kinase MARK2	Kinase	Q7KZI7	MARK2_HUMAN		Kd	7	CHEMBL
Hepatocyte growth factor receptor	Kinase	P08581	MET_HUMAN		Kd	6.25	CHEMBL
Tyrosine-protein kinase Lyn	Kinase	P07948	LYN_HUMAN		Kd	5.38	CHEMBL
Ribosomal protein S6 kinase alpha-2	Kinase	Q15349	KS6A2_HUMAN		Kd	6.62	CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-1	Kinase	Q13131	AAPK1_HUMAN		Kd	6.75	CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit beta	Kinase	Q13554	KCC2B_HUMAN		Kd	6.68	CHEMBL
Protein kinase C eta type	Kinase	P24723	KPCL_HUMAN		Kd	6.54	CHEMBL
Fibroblast growth factor receptor 1	Kinase	P11362	FGFR1_HUMAN		Kd	5.80	CHEMBL
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform	Kinase	Q16816	PHKG1_HUMAN		Kd	6.72	CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit alpha	Kinase	Q9UQM7	KCC2A_HUMAN		Kd	7.70	CHEMBL
Serine/threonine-protein kinase 17B	Kinase	O94768	ST17B_HUMAN		Kd	5.33	CHEMBL
Serine/threonine-protein kinase 10	Kinase	O94804	STK10_HUMAN		Kd	6.23	CHEMBL
Tyrosine-protein kinase Fer	Kinase	P16591	FER_HUMAN		Kd	5.92	CHEMBL
Protein kinase C epsilon type	Kinase	Q02156	KPCE_HUMAN		Kd	6.27	CHEMBL
Serine/threonine-protein kinase PLK4	Kinase	O00444	PLK4_HUMAN		Kd	7.18	CHEMBL
Aurora kinase C	Kinase	Q9UQB9	AURKC_HUMAN		Kd	6.77	CHEMBL
Serine/threonine-protein kinase 16	Kinase	O75716	STK16_HUMAN		Kd	6.55	CHEMBL
Dual specificity protein kinase TTK	Kinase	P33981	TTK_HUMAN		Kd	6.46	CHEMBL
Fibroblast growth factor receptor 2	Kinase	P21802	FGFR2_HUMAN		Kd	5.62	CHEMBL
Serine/threonine-protein kinase N1	Kinase	Q16512	PKN1_HUMAN		Kd	8.03	CHEMBL
Protein kinase C theta type	Kinase	Q04759	KPCT_HUMAN		Kd	6.04	CHEMBL
Serine/threonine-protein kinase 17A	Kinase	Q9UEE5	ST17A_HUMAN		Kd	5.72	CHEMBL
TRAF2 and NCK-interacting protein kinase	Kinase	Q9UKE5	TNIK_HUMAN		Kd	5.80	CHEMBL
Tyrosine-protein kinase Fgr	Kinase	P09769	FGR_HUMAN		Kd	6.14	CHEMBL
Aurora kinase A	Kinase	O14965	AURKA_HUMAN		IC50	7.10	CHEMBL
ALK tyrosine kinase receptor	Kinase	Q9UM73	ALK_HUMAN		Kd	6.57	CHEMBL
RAC-alpha serine/threonine-protein kinase	Kinase	P31749	AKT1_HUMAN		Kd	6.02	CHEMBL
BMP-2-inducible protein kinase	Kinase	Q9NSY1	BMP2K_HUMAN		Kd	6.66	CHEMBL
Serine/threonine-protein kinase pim-2	Kinase	Q9P1W9	PIM2_HUMAN		Kd	5.51	CHEMBL
Tyrosine-protein kinase FRK	Kinase	P42685	FRK_HUMAN		Kd	5.62	CHEMBL
Dual specificity protein kinase CLK1	Kinase	P49759	CLK1_HUMAN		Kd	6.46	CHEMBL
Dual specificity protein kinase CLK2	Kinase	P49760	CLK2_HUMAN		Kd	6.07	CHEMBL
Dual specificity protein kinase CLK3	Kinase	P49761	CLK3_HUMAN		Kd	5.44	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5	Kinase	Q9Y4K4	M4K5_HUMAN		Kd	5.96	CHEMBL
Cyclin-G-associated kinase	Kinase	O14976	GAK_HUMAN		Kd	6.42	CHEMBL
Glycogen synthase kinase-3 beta	Kinase	P49841	GSK3B_HUMAN		Kd	5.75	CHEMBL
Calcium/calmodulin-dependent protein kinase type 1D	Kinase	Q8IU85	KCC1D_HUMAN		Kd	6.17	CHEMBL
Serine/threonine-protein kinase 4	Kinase	Q13043	STK4_HUMAN		Kd	7.77	CHEMBL
Activated CDC42 kinase 1	Kinase	Q07912	ACK1_HUMAN		Kd	6.92	CHEMBL
Ribosomal protein S6 kinase alpha-5	Kinase	O75582	KS6A5_HUMAN		Kd	6.62	CHEMBL
STE20-like serine/threonine-protein kinase	Kinase	Q9H2G2	SLK_HUMAN		Kd	6.66	CHEMBL
Dual specificity protein kinase CLK4	Kinase	Q9HAZ1	CLK4_HUMAN		Kd	6.39	CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 2	Kinase	Q9HBH9	MKNK2_HUMAN		Kd	6.02	CHEMBL
Mitogen-activated protein kinase 9	Kinase	P45984	MK09_HUMAN		Kd	5.30	CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2	Kinase	Q96RR4	KKCC2_HUMAN		Kd	7.14	CHEMBL
MAP/microtubule affinity-regulating kinase 3	Kinase	P27448	MARK3_HUMAN		Kd	7.68	CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 1	Kinase	Q8N5S9	KKCC1_HUMAN		Kd	6.89	CHEMBL
Calcium/calmodulin-dependent protein kinase type 1G	Kinase	Q96NX5	KCC1G_HUMAN		Kd	5.75	CHEMBL
Epithelial discoidin domain-containing receptor 1	Kinase	Q08345	DDR1_HUMAN		Kd	5.14	CHEMBL
Testis-specific serine/threonine-protein kinase 1	Kinase	Q9BXA7	TSSK1_HUMAN		Kd	5.32	CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit beta	Kinase	O14920	IKKB_HUMAN		Kd	5.20	CHEMBL
3-phosphoinositide-dependent protein kinase 1	Kinase	O15530	PDPK1_HUMAN		Kd	6.96	CHEMBL
Tyrosine-protein kinase ZAP-70	Kinase	P43403	ZAP70_HUMAN		Kd	5.59	CHEMBL
Glycogen synthase kinase-3 alpha	Kinase	P49840	GSK3A_HUMAN		Kd	5.60	CHEMBL
Tyrosine-protein kinase receptor UFO	Kinase	P30530	UFO_HUMAN		Kd	6.21	CHEMBL
BDNF/NT-3 growth factors receptor	Kinase	Q16620	NTRK2_HUMAN		Kd	6.51	CHEMBL
Tyrosine-protein kinase receptor TYRO3	Kinase	Q06418	TYRO3_HUMAN		Kd	7.06	CHEMBL
Ribosomal protein S6 kinase beta-1	Kinase	P23443	KS6B1_HUMAN		Kd	5.89	CHEMBL
Serine/threonine-protein kinase N2	Kinase	Q16513	PKN2_HUMAN		Kd	7.82	CHEMBL
RAC-beta serine/threonine-protein kinase	Kinase	P31751	AKT2_HUMAN		Kd	6.11	CHEMBL
Serine/threonine-protein kinase 3	Kinase	Q13188	STK3_HUMAN		Kd	7.40	CHEMBL
Ribosomal protein S6 kinase alpha-6	Kinase	Q9UK32	KS6A6_HUMAN		Kd	5.82	CHEMBL
NUAK family SNF1-like kinase 2	Kinase	Q9H093	NUAK2_HUMAN		Kd	7.20	CHEMBL
Non-receptor tyrosine-protein kinase TNK1	Kinase	Q13470	TNK1_HUMAN		Kd	7.08	CHEMBL
Non-receptor tyrosine-protein kinase TYK2	Kinase	P29597	TYK2_HUMAN		Kd	6.60	CHEMBL
Serine/threonine-protein kinase Chk1	Kinase	O14757	CHK1_HUMAN		Kd	5.89	CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform	Kinase	P42336	PK3CA_HUMAN		Kd	5.96	CHEMBL
Serine/threonine-protein kinase PAK 3	Kinase	O75914	PAK3_HUMAN		Kd	6.75	CHEMBL
Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha	Kinase	Q99755	PI51A_HUMAN		Kd	6.51	CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 beta	Kinase	P78356	PI42B_HUMAN		Kd	6.57	CHEMBL
Myosin light chain kinase family member 4	Kinase	Q86YV6	MYLK4_HUMAN		Kd	6.19	CHEMBL
Wee1-like protein kinase	Kinase	P30291	WEE1_HUMAN		Kd	5.34	CHEMBL
Serine/threonine-protein kinase 25	Kinase	O00506	STK25_HUMAN		Kd	5.75	CHEMBL
Protein-tyrosine kinase 2-beta	Kinase	Q14289	FAK2_HUMAN		Kd	6.18	CHEMBL
Serine/threonine-protein kinase RIO1	Kinase	Q9BRS2	RIOK1_HUMAN		Kd	5.92	CHEMBL
Tyrosine-protein kinase receptor Tie-1	Kinase	P35590	TIE1_HUMAN		Kd	5.85	CHEMBL
NT-3 growth factor receptor	Kinase	Q16288	NTRK3_HUMAN		Kd	5.77	CHEMBL
Casein kinase II subunit alpha	Kinase	P68400	CSK21_HUMAN		Kd	6.60	CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1B	Kinase	Q9Y463	DYR1B_HUMAN		Kd	6.48	CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon	Kinase	Q14164	IKKE_HUMAN		Kd	6.80	CHEMBL
Serine/threonine-protein kinase STK11	Kinase	Q15831	STK11_HUMAN		Kd	6.46	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 3	Kinase	P46734	MP2K3_HUMAN		Kd	5.28	CHEMBL
Maternal embryonic leucine zipper kinase	Kinase	Q14680	MELK_HUMAN		Kd	6.55	CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 4	Kinase	Q9P2K8	E2AK4_HUMAN		Kd	7.41	CHEMBL
Interleukin-1 receptor-associated kinase 3	Kinase	Q9Y616	IRAK3_HUMAN		Kd	6.75	CHEMBL
Serine/threonine-protein kinase RIO3	Kinase	O14730	RIOK3_HUMAN		Kd	6.38	CHEMBL
Serine/threonine-protein kinase SIK2	Kinase	Q9H0K1	SIK2_HUMAN		Kd	6.25	CHEMBL
SRSF protein kinase 1	Kinase	Q96SB4	SRPK1_HUMAN		Kd	7.38	CHEMBL
SRSF protein kinase 2	Kinase	P78362	SRPK2_HUMAN		Kd	6.48	CHEMBL
Serine/threonine-protein kinase 33	Kinase	Q9BYT3	STK33_HUMAN		Kd	6.72	CHEMBL
5'-AMP-activated protein kinase catalytic subunit alpha-2	Kinase	P54646	AAPK2_HUMAN		Kd	6.34	CHEMBL
Myotonin-protein kinase	Kinase	Q09013	DMPK_HUMAN		Kd	5.42	CHEMBL
RAC-gamma serine/threonine-protein kinase	Kinase	Q9Y243	AKT3_HUMAN		Kd	5.36	CHEMBL
Serine/threonine-protein kinase LATS1	Kinase	O95835	LATS1_HUMAN		Kd	5.96	CHEMBL
Serine/threonine-protein kinase LATS2	Kinase	Q9NRM7	LATS2_HUMAN		Kd	5.66	CHEMBL
Leukocyte tyrosine kinase receptor	Kinase	P29376	LTK_HUMAN		Kd	5.52	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1	Kinase	Q92918	M4K1_HUMAN		Kd	5.68	CHEMBL
NUAK family SNF1-like kinase 1	Kinase	O60285	NUAK1_HUMAN		Kd	7.39	CHEMBL
Serine/threonine-protein kinase pim-3	Kinase	Q86V86	PIM3_HUMAN		Kd	6.25	CHEMBL
cAMP-dependent protein kinase catalytic subunit alpha	Kinase	P17612	KAPCA_HUMAN		Kd	6.14	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3	Kinase	Q8IVH8	M4K3_HUMAN		Kd	6.92	CHEMBL
Aurora kinase B	Kinase	Q96GD4	AURKB_HUMAN		Kd	7.21	CHEMBL
Tyrosine-protein kinase Blk	Kinase	P51451	BLK_HUMAN		Kd	6.30	CHEMBL
Serine/threonine-protein kinase BRSK1	Kinase	Q8TDC3	BRSK1_HUMAN		Kd	5.92	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4	Kinase	O95819	M4K4_HUMAN		Kd	6.19	CHEMBL
Serine/threonine-protein kinase MARK1	Kinase	Q9P0L2	MARK1_HUMAN		Kd	6.77	CHEMBL
MAP/microtubule affinity-regulating kinase 4	Kinase	Q96L34	MARK4_HUMAN		Kd	6.43	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 4	Kinase	P45985	MP2K4_HUMAN		Kd	5.32	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 6	Kinase	P52564	MP2K6_HUMAN		Kd	5.19	CHEMBL
Tyrosine-protein kinase Mer	Kinase	Q12866	MERTK_HUMAN		Kd	5.54	CHEMBL
Cyclin-dependent kinase 19	Kinase	Q9BWU1	CDK19_HUMAN		Kd	5.14	CHEMBL
Mitogen-activated protein kinase kinase kinase 9	Kinase	P80192	M3K9_HUMAN		Kd	7.82	CHEMBL
Mitogen-activated protein kinase kinase kinase 10	Kinase	Q02779	M3K10_HUMAN		Kd	6.10	CHEMBL
Mitogen-activated protein kinase kinase kinase 11	Kinase	Q16584	M3K11_HUMAN		Kd	7.77	CHEMBL
Death-associated protein kinase 1	Kinase	P53355	DAPK1_HUMAN		Kd	5.33	CHEMBL
Serine/threonine-protein kinase PAK 1	Kinase	Q13153	PAK1_HUMAN		Kd	5.70	CHEMBL
Serine/threonine-protein kinase PAK 2	Kinase	Q13177	PAK2_HUMAN		Kd	5.68	CHEMBL
Serine/threonine-protein kinase BRSK2	Kinase	Q8IWQ3	BRSK2_HUMAN		Kd	6.19	CHEMBL
Serine/threonine-protein kinase SIK1	Kinase	P57059	SIK1_HUMAN		Kd	6.80	CHEMBL
Serine/threonine-protein kinase D2	Kinase	Q9BZL6	KPCD2_HUMAN		Kd	5.20	CHEMBL
Serine/threonine-protein kinase D3	Kinase	O94806	KPCD3_HUMAN		Kd	5.50	CHEMBL
cGMP-dependent protein kinase 2	Kinase	Q13237	KGP2_HUMAN		Kd	7.13	CHEMBL
Interferon-induced, double-stranded RNA-activated protein kinase	Kinase	P19525	E2AK2_HUMAN		Kd	5.16	CHEMBL
Proto-oncogene tyrosine-protein kinase ROS	Kinase	P08922	ROS1_HUMAN		Kd	6.37	CHEMBL
Ribosomal protein S6 kinase alpha-1	Kinase	Q15418	KS6A1_HUMAN		Kd	6.59	CHEMBL
Ribosomal protein S6 kinase alpha-4	Kinase	O75676	KS6A4_HUMAN		Kd	6.59	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2	Kinase	Q12851	M4K2_HUMAN		Kd	5.60	CHEMBL
Misshapen-like kinase 1	Kinase	Q8N4C8	MINK1_HUMAN		Kd	6.77	CHEMBL
Serine/threonine-protein kinase TBK1	Kinase	Q9UHD2	TBK1_HUMAN		Kd	8.03	CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1A	Kinase	Q13627	DYR1A_HUMAN		Kd	7	CHEMBL
Ephrin type-B receptor 6	Kinase	O15197	EPHB6_HUMAN		Kd	5.51	CHEMBL
Serine/threonine-protein kinase/endoribonuclease IRE1	Kinase	O75460	ERN1_HUMAN		Kd	5.64	CHEMBL
Rhodopsin kinase	Kinase	Q15835	RK_HUMAN		Kd	7.07	CHEMBL
G protein-coupled receptor kinase 4	Kinase	P32298	GRK4_HUMAN		Kd	6.96	CHEMBL
G protein-coupled receptor kinase 7	Kinase	Q8WTQ7	GRK7_HUMAN		Kd	7.32	CHEMBL
Homeodomain-interacting protein kinase 2	Kinase	Q9H2X6	HIPK2_HUMAN		Kd	5.51	CHEMBL
Homeodomain-interacting protein kinase 3	Kinase	Q9H422	HIPK3_HUMAN		Kd	5.64	CHEMBL
Homeodomain-interacting protein kinase 4	Kinase	Q8NE63	HIPK4_HUMAN		Kd	6.02	CHEMBL
Hormonally up-regulated neu tumor-associated kinase	Kinase	P57058	HUNK_HUMAN		Kd	6.62	CHEMBL
Serine/threonine-protein kinase ICK	Kinase	Q9UPZ9	ICK_HUMAN		Kd	5.23	CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit alpha	Kinase	O15111	IKKA_HUMAN		Kd	5.42	CHEMBL
Mitogen-activated protein kinase kinase kinase 13	Kinase	O43283	M3K13_HUMAN		Kd	5.55	CHEMBL
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform	Kinase	P15735	PHKG2_HUMAN		Kd	6.05	CHEMBL
Mitogen-activated protein kinase kinase kinase 3	Kinase	Q99759	M3K3_HUMAN		Kd	6.68	CHEMBL
Microtubule-associated serine/threonine-protein kinase 1	Kinase	Q9Y2H9	MAST1_HUMAN		Kd	6.72	CHEMBL
U4/U6 small nuclear ribonucleoprotein Prp4	Nuclear other	O43172	PRP4_HUMAN		Kd	7.26	CHEMBL
Serine/threonine-protein kinase RIO2	Kinase	Q9BVS4	RIOK2_HUMAN		Kd	7.01	CHEMBL
SRSF protein kinase 3	Kinase	Q9UPE1	SRPK3_HUMAN		Kd	7.10	CHEMBL
Mitogen-activated protein kinase kinase kinase 7	Kinase	O43318	M3K7_HUMAN		Kd	6.89	CHEMBL
Serine/threonine-protein kinase ULK3	Kinase	Q6PHR2	ULK3_HUMAN		Kd	5.89	CHEMBL
Mitogen-activated protein kinase kinase kinase 19	Kinase	Q56UN5	M3K19_HUMAN		Kd	7.82	CHEMBL
Tankyrase-2	Enzyme	Q9H2K2	TNKS2_HUMAN		Kd	6.92	CHEMBL
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Kinase	O00750	P3C2B_HUMAN		Kd	5.85	CHEMBL
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma	Kinase	O75747	P3C2G_HUMAN		Kd	6.24	CHEMBL
Serine/threonine-protein kinase SIK3	Kinase	Q9Y2K2	SIK3_HUMAN		Kd	7.01	CHEMBL
Serine/threonine-protein kinase 32A	Kinase	Q8WU08	ST32A_HUMAN		Kd	5.62	CHEMBL
Serine/threonine-protein kinase PRP4 homolog	Kinase	Q13523	PRP4B_HUMAN		Kd	7.26	CHEMBL
Serine/threonine-protein kinase Sgk3	Kinase	Q96BR1	SGK3_HUMAN		Kd	5.85	CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 1	Kinase	Q9BQI3	E2AK1_HUMAN		Kd	5.69	CHEMBL
Myosin light chain kinase 3	Kinase	Q32MK0	MYLK3_HUMAN		Kd	5.64	CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2	Kinase	Q5S007	LRRK2_HUMAN		Kd	6.75	CHEMBL
Dual serine/threonine and tyrosine protein kinase	Kinase	Q6XUX3	DUSTY_HUMAN		Kd	5.33	CHEMBL
cGMP-dependent protein kinase 1	Kinase	Q13976	KGP1_HUMAN		Kd	6.60	CHEMBL
cAMP-dependent protein kinase catalytic subunit PRKX	Kinase	P51817	PRKX_HUMAN		Kd	6.02	CHEMBL
5'-AMP-activated protein kinase subunit gamma-1	Kinase	P54619	AAKG1_HUMAN		Kd	5.93	CHEMBL
Uncharacterized protein FLJ45252	Unclassified	Q6ZSR9	YJ005_HUMAN		Kd	6.53	CHEMBL
5'-AMP-activated protein kinase subunit gamma-2	Kinase	Q9UGJ0	AAKG2_HUMAN		Kd	5.04	CHEMBL
Mitogen-activated protein kinase kinase kinase 2	Kinase	Q9Y2U5	M3K2_HUMAN		Kd	6.85	CHEMBL
Tubulin alpha-1A chain	Structural		TBA1A_RAT		Kd	5.51	CHEMBL
Calcium-dependent protein kinase 1	Kinase		CDPK1_PLAF7		Kd	6.02	CHEMBL

External reference:

ID	Source
ID912S5VON	UNII
4036652	VANDF
C0526371	UMLSCUI
CHEBI:63452	CHEBI
2K2	PDB_CHEM_ID
CHEMBL608533	ChEMBL_ID
9829523	PUBCHEM_CID
DB06595	DRUGBANK_ID
D05029	KEGG_DRUG
7677	INN_ID
5702	IUPHAR_LIGAND_ID
256612	MMSL
32671	MMSL
d08575	MMSL
017198	NDDF
763613005	SNOMEDCT_US
763614004	SNOMEDCT_US
1919083	RXNORM
C059539	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
RYDAPT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0698	CAPSULE, LIQUID FILLED	25 mg	ORAL	NDA	28 sections
RYDAPT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0698	CAPSULE, LIQUID FILLED	25 mg	ORAL	NDA	28 sections
RYDAPT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0698	CAPSULE, LIQUID FILLED	25 mg	ORAL	NDA	28 sections