GPCRdb

GR 127935

Agent/drug
Bioactivity

GR 127935

SMILES	COc1ccc(NC(=O)c2ccc(-c3ccc(-c4noc(C)n4)cc3C)cc2)cc1N1CCN(C)CC1
InChIKey	YDBCEBYHYKAFRX-UHFFFAOYSA-N

Chemical Properties

Hydrogen bond acceptors	7
Hydrogen bond donors	1
Rotatable bonds	6
Molecular weight (Da)	497.2

Database connections

PubChem Guide To Pharmacology ChEMBL_compound_ids GPCRdb

Bioactivities

Affinity
Potency

Search:

Receptor					Activity				Source

Protein	Gene	Species	Family	Class	Type	Min	Avg	Max	Database

5-HT_1A	5HT1A	Human	5-Hydroxytryptamine	A	pKi	7.10	7.15	7.20	Guide to Pharmacology
5-HT_1A	5HT1A	Rat	5-Hydroxytryptamine	A	pKi	6.50	6.50	6.50	ChEMBL
5-HT_1A	5HT1A	Human	5-Hydroxytryptamine	A	pKi	7.10	7.13	7.16	ChEMBL
5-HT_1A	5HT1A	Human	5-Hydroxytryptamine	A	pKi	7.10	7.15	7.20	PDSP Ki database
5-HT_1B	5HT1B	Human	5-Hydroxytryptamine	A	pKi	9.00	9.30	9.80	Guide to Pharmacology
5-HT_1B	5HT1B	Rat	5-Hydroxytryptamine	A	pKi	8.50	8.50	8.50	ChEMBL
5-HT_1B	5HT1B	Human	5-Hydroxytryptamine	A	pKi	8.37	9.27	9.85	ChEMBL
5-HT_1B	5HT1B	Human	5-Hydroxytryptamine	A	pKi	8.10	8.94	9.85	PDSP Ki database
5-HT_1B	5HT1B	Rat	5-Hydroxytryptamine	A	pKi	8.22	8.36	8.50	PDSP Ki database
5-HT_1B	5HT1B	Guinea pig	5-Hydroxytryptamine	A	pKi	8.37	8.37	8.37	PDSP Ki database
5-HT_1D	5HT1D	Human	5-Hydroxytryptamine	A	pKi	8.30	8.65	9.10	Guide to Pharmacology
5-HT_1D	5HT1D	Guinea pig	5-Hydroxytryptamine	A	pKi	8.50	8.50	8.50	ChEMBL
5-HT_1D	5HT1D	Human	5-Hydroxytryptamine	A	pKi	7.91	8.94	9.90	ChEMBL
5-HT_1D	5HT1D	Human	5-Hydroxytryptamine	A	pKi	7.91	8.82	9.92	PDSP Ki database
5-HT_1E	5HT1E	Human	5-Hydroxytryptamine	A	pKi	5.40	5.40	5.40	Guide to Pharmacology
5-HT_1E	5HT1E	Human	5-Hydroxytryptamine	A	pKi	5.40	5.40	5.40	PDSP Ki database
5-HT_1F	5HT1F	Human	5-Hydroxytryptamine	A	pKi	6.40	6.80	7.20	Guide to Pharmacology
5-HT_1F	5HT1F	Human	5-Hydroxytryptamine	A	pKi	6.40	6.40	6.40	PDSP Ki database
5-HT_2A	5HT2A	Human	5-Hydroxytryptamine	A	pKi	7.80	7.80	7.80	Guide to Pharmacology
5-HT_2A	5HT2A	Human	5-Hydroxytryptamine	A	pKi	7.37	7.58	7.80	PDSP Ki database

Showing 1 to 20 of 32 entries

Search:

Receptor					Activity				Source

Protein	Gene	Species	Family	Class	Type	Min	Avg	Max	Database

5-HT_1A	5HT1A	Rat	5-Hydroxytryptamine	A	pIC50	6.37	6.41	6.44	ChEMBL
5-HT_1B	5HT1B	Rat	5-Hydroxytryptamine	A	pIC50	8.80	8.80	8.80	ChEMBL
5-HT_1D	5HT1D	Human	5-Hydroxytryptamine	A	pIC50	7.28	7.28	7.28	ChEMBL
5-HT_1D	5HT1D	Rat	5-Hydroxytryptamine	A	pIC50	7.28	7.28	7.28	ChEMBL
M₁	ACM1	Rat	Acetylcholine (muscarinic)	A	Potency	4.50	4.67	4.85	ChEMBL
NPS	NPSR1	Human	Neuropeptide S	A	Potency	4.80	4.80	4.80	ChEMBL
TSH	TSHR	Human	Glycoprotein hormone	A	Potency	5.20	5.20	5.20	ChEMBL

Showing 1 to 7 of 7 entries

GR 127935

Drug properties

Molecular type	Small molecule
Physiological/Surrogate	Surrogate
Approved drug	No

Distribution across phases (no. indications)

Phase I 0

Phase II 0

Phase III 0

Phase IV

Database connections

PubChem Guide To Pharmacology ChEMBL_compound_ids GPCRdb

Compound is not listed as a drug.