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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 |
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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 27:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]