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| Stem definition | Drug id | CAS RN |
|---|---|---|
| melanocortin receptor agonists; peptides and glycopeptides | 5329 | 189691-06-3 |
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| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -0.585 | High | 0.80 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.611 | High | 0.80 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.342 | 10^-6 cm/s | High | 0.80 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.303 | uL/min/10^6 cells | High | 0.80 |
| dppb | Dog plasma protein binding (% unbound) | 81.330 | % | High | 0.80 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 44.670 | % | High | 0.80 |
| herg | hERG pIC50 | 4.588 | pIC50 | High | 0.80 |
| hh-clint | Human hepatocyte intrinsic clearance | 3.597 | uL/min/10^6 cells | High | 0.80 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.141 | uL/min/mg protein | High | 0.80 |
| hppb | Human plasma protein binding (% unbound) | 81.810 | % | High | 0.80 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,PDK1,PDK2,PRKDC | 14 | |||
| kinase-selectivity-class | AXL,GRK2 | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.324 | High | 0.80 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 5.117 | High | 0.80 | |
| mppb | Mouse plasma protein binding (% unbound) | 68.330 | High | 0.80 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.242 | High | 0.80 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 69.120 | % | High | 0.80 |
| rh-clint | Rat hepatocyte intrinsic clearance | 3.508 | uL/min/10^6 cells | High | 0.80 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 76.480 | % | High | 0.80 |
| rppb | Rat plasma protein binding (% unbound) | 67.070 | % | High | 0.80 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 883.080 | uM | High | 0.80 |
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 21, 2019 | FDA | AMAG PHARMS INC |
| 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 |
|---|---|---|---|---|---|---|
| Nausea | 101.10 | 65.38 | 45 | 126 | 1110271 | 89518005 |
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| Source | Code | Description |
|---|---|---|
| ATC | G02CX05 | GENITO URINARY SYSTEM AND SEX HORMONES OTHER GYNECOLOGICALS OTHER GYNECOLOGICALS Other gynecologicals |
| FDA EPC | N0000194029 | Melanocortin Receptor Agonist |
| FDA MoA | N0000194030 | Melanocortin Receptor Agonists |
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Lack or loss of sexual desire | indication | 270903007 | DOID:13868 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
None
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| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.28 | acidic |
| pKa2 | 12.41 | acidic |
| pKa3 | 12.76 | acidic |
| pKa4 | 13.11 | acidic |
| pKa5 | 13.39 | acidic |
| pKa6 | 13.66 | acidic |
| pKa7 | 8.36 | Basic |
| pKa8 | 7.73 | Basic |
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 1.75MG BASE/0.3ML (EQ 1.75MG BASE/0.3 ML) | VYLEESI (AUTOINJECTOR) | COSETTE | N210557 | June 21, 2019 | RX | SOLUTION | SUBCUTANEOUS | 10286034 | Nov. 5, 2033 | TREATMENT OF HYPOACTIVE SEXUAL DESIRE DISORDER (HSDD) |
| EQ 1.75MG BASE/0.3ML (EQ 1.75MG BASE/0.3 ML) | VYLEESI (AUTOINJECTOR) | COSETTE | N210557 | June 21, 2019 | RX | SOLUTION | SUBCUTANEOUS | 9352013 | Nov. 5, 2033 | TREATMENT OF HYPOACTIVE SEXUAL DESIRE DISORDER (HSDD) |
| EQ 1.75MG BASE/0.3ML (EQ 1.75MG BASE/0.3 ML) | VYLEESI (AUTOINJECTOR) | COSETTE | N210557 | June 21, 2019 | RX | SOLUTION | SUBCUTANEOUS | 9700592 | Nov. 5, 2033 | TREATMENT OF HYPOACTIVE SEXUAL DESIRE DISORDER (HSDD) |
| EQ 1.75MG BASE/0.3ML (EQ 1.75MG BASE/0.3 ML) | VYLEESI (AUTOINJECTOR) | COSETTE | N210557 | June 21, 2019 | RX | SOLUTION | SUBCUTANEOUS | 11590209 | April 29, 2041 | TREATING ACQUIRED, GENERALIZED HYPOACTIVE SEXUAL DESIRE DISORDER (HSDD) IN A PREMENOPAUSAL FEMALE PATIENT WITH CONTROLLED HYPERTENSION BY INJECTING BREMELANOTIDE MORE THAN ONCE WITH AT LEAST 24 HOURS BETWEEN DOSES AND NO MORE THAN 8 DOSES PER MONTH |
None
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Melanocortin receptor 4 | GPCR | AGONIST | Kd | 8 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Melanocortin receptor 5 | GPCR | AGONIST | Ki | 7.77 | CHEMBL | ||||
| Melanocortin receptor 3 | GPCR | AGONIST | EC50 | 8.62 | CHEMBL | ||||
| Melanocyte-stimulating hormone receptor | GPCR | AGONIST | EC50 | 10.02 | CHEMBL | ||||
| Adrenocorticotropic hormone receptor | GPCR | AGONIST | DRUG LABEL |
| ID | Source |
|---|---|
| 6Y24O4F92S | UNII |
| 1607799-13-2 | SECONDARY_CAS_RN |
| 4038620 | VANDF |
| C1721339 | UMLSCUI |
| CHEMBL2070241 | ChEMBL_ID |
| 9941379 | PUBCHEM_CID |
| DB11653 | DRUGBANK_ID |
| CHEMBL4297533 | ChEMBL_ID |
| D06569 | KEGG_DRUG |
| 8737 | INN_ID |
| C476721 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10408 | IUPHAR_LIGAND_ID |
| 427418003 | SNOMEDCT_US |
| 788500001 | SNOMEDCT_US |
| CHEBI:757011 | CHEBI |
| 37138 | MMSL |
| d09322 | MMSL |
| 018059 | NDDF |
| 018060 | NDDF |
| 2176311 | RXNORM |
| 6Y24O4F92S | INXIGHT DRUGS |
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Vyleesi | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0713-0897 | INJECTION | 1.75 mg | SUBCUTANEOUS | NDA | 27 sections |