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 35:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
