PD-135666 [Ligand Id: 903] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL138534 (PD-135666)
  • CCK1 receptor/Cholecystokinin A receptor in Rat [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551]
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  • CCK2 receptor/Cholecystokinin B receptor in Mouse [ChEMBL: CHEMBL2854] [GtoPdb: 77] [UniProtKB: P56481]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CCK1 receptor/Cholecystokinin A receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551]
ChEMBL Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas. B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (1993) 3: 989-992
ChEMBL Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas B 7.59 pIC50 25.5 nM IC50 J Med Chem (1998) 41: 38-45 [PMID:9438020]
ChEMBL Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas B 7.59 pIC50 25.5 nM IC50 J Med Chem (2000) 43: 3505-3517 [PMID:11000005]
ChEMBL Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas B 7.59 pIC50 25.5 nM IC50 Bioorg Med Chem Lett (1993) 3: 881-884
CCK2 receptor/Cholecystokinin B receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2854] [GtoPdb: 77] [UniProtKB: P56481]
ChEMBL Cholecystokinin type B receptor binding assay performed on homogenized cerebral cortex from male mouse B 9.83 pKi 0.15 nM Ki J Med Chem (1992) 35: 1572-1577 [PMID:1578483]
GtoPdb - - 9.8 pIC50 - - - Eur J Pharmacol (1995) 286: 185-91 [PMID:8605955]
ChEMBL Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type B receptor in the mouse cerebral cortex B 9.82 pIC50 0.15 nM IC50 J Med Chem (1998) 41: 38-45 [PMID:9438020]
ChEMBL Half maximal inhibition of specific binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type B receptor in the mouse cerebral cortex B 9.82 pIC50 0.15 nM IC50 J Med Chem (2000) 43: 3505-3517 [PMID:11000005]
ChEMBL Compound measured for half-maximal inhibition of specific binding of [125I]bolton Hunter CCK-26-33 to CCK-B receptor in the mouse cerebral cortex. B 9.82 pIC50 0.15 nM IC50 Bioorg Med Chem Lett (1993) 3: 989-992
ChEMBL Inhibition of [125I]CCK-8 to Cholecystokinin type B receptor in the mouse cerebral cortex. B 9.82 pIC50 0.15 nM IC50 Bioorg Med Chem Lett (1993) 3: 881-884

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]