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 31:

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]