3-APMPA [Ligand Id: 1080] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL112710 (CGP-35024)
1 CHEMBL112710_lig_chart_1 GABA B receptor Rat
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2 CHEMBL112710_lig_chart_2 GABA-B receptor Human
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  • GABAB1/GABA-B receptor 1 in Rat [ChEMBL: CHEMBL2753] [GtoPdb: 240] [UniProtKB: Q9Z0U4]
  • This target only has 0 pki data point
3 CHEMBL112710_lig_chart_3 GABA-B receptor 1 Rat
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  • GABAB receptor in Human [GtoPdb: 242]
  • GABAB receptor in Rat [GtoPdb: 242]
  • This target only has 1 pki data point
4 CHEMBL112710_lig_chart_4 GABAB receptor HumanRat
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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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]