3-APMPA [Ligand Id: 1080] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL112710 (CGP-35024) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GABAB2/GABAB1/GABA B receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111474] [GtoPdb: 241, 240] [UniProtKB: O88871, Q9Z0U4] | ||||||||
| ChEMBL | In vitro displacement of [3H]GABA from Gamma-aminobutyric acid type B receptor sites in rat brain membranes | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 515-518 |
| ChEMBL | Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortex | B | 10.8 | pIC50 | 0.02 | nM | IC50 | J Med Chem (1995) 38: 3297-3312 [PMID:7650684] |
| GABAB2/GABAB1/GABA-B receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111463] [GtoPdb: 241, 240] [UniProtKB: O75899, Q9UBS5] | ||||||||
| ChEMBL | Inhibition of [3H]-baclofen binding to Gamma-aminobutyric acid type B receptor of cat cerebellum | B | 8.18 | pIC50 | 6.6 | nM | IC50 | J Med Chem (1995) 38: 3297-3312 [PMID:7650684] |
| ChEMBL | Inhibition of mammalian Gamma-aminobutyric acid type B receptor (potent agonist) | F | 6.7 | pEC50 | 200 | nM | EC50 | Bioorg Med Chem Lett (1996) 6: 2073-2076 |
| GABAB1/GABA-B receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2753] [GtoPdb: 240] [UniProtKB: Q9Z0U4] | ||||||||
| ChEMBL | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (1995) 38: 3313-3331 [PMID:7650685] |
| GABAB receptor in Human [GtoPdb: 242] | ||||||||
| GtoPdb | - | - | 5.1 | pKi | - | - | - | Br J Pharmacol (2000) 131: 1050-4 [PMID:11082110] |
| GABAB receptor in Rat [GtoPdb: 242] | ||||||||
| GtoPdb | - | - | 8.2 | pIC50 | - | - | - | Chemistry of GABAB modulators.. The GABA Receptors (1997) |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
