CE-326597 [Ligand Id: 9055] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1269258 (Ce-326,597, Ce-326597, CE-326,597)
  • CCK1 receptor/Cholecystokinin A receptor in Human [ChEMBL: CHEMBL1901] [GtoPdb: 76] [UniProtKB: P32238]
  • CCK1 receptor/Cholecystokinin A receptor in Rat [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551]
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  • CCK2 receptor/Cholecystokinin B receptor in Human [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239]
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1901] [GtoPdb: 76] [UniProtKB: P32238]
ChEMBL Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter B 6.37 pKi 426.58 nM Ki J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter B 6.56 pKi 275.42 nM Ki J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counter B 6.78 pKi 165.96 nM Ki J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counter B 7.61 pKi 24.55 nM Ki J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter B 6 pIC50 1000 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-1] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counter B 6 pIC50 >1000 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter B 6.1 pIC50 794.33 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counter B 6.17 pIC50 676.08 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter B 6.2 pIC50 634 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter B 6.21 pIC50 616.6 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counter B 6.57 pIC50 269.15 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter B 6.78 pIC50 165.96 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Agonist activity at human CCK1R W6.48A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis F 7 pIC50 >100 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter B 7.03 pIC50 93.33 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter B 7.37 pIC50 42.66 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counter B 7.38 pIC50 41.69 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counter B 7.43 pIC50 37.15 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells B 7.5 pIC50 31.7 nM IC50 Bioorg Med Chem Lett (2010) 20: 6797-6801 [PMID:20851601]
GtoPdb - - 7.5 pIC50 31.7 nM IC50 Bioorg Med Chem Lett (2010) 20: 6797-801 [PMID:20851601]
ChEMBL Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter B 7.57 pIC50 26.8 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting B 7.63 pIC50 23.6 nM IC50 Bioorg Med Chem Lett (2012) 22: 2943-2947 [PMID:22424974]
ChEMBL Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter B 7.65 pIC50 22.39 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter B 7.78 pIC50 16.6 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter B 7.82 pIC50 15.14 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counter B 8.35 pIC50 4.47 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Agonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis F 8.51 pIC50 3.09 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter B 8.7 pIC50 2 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay F 6.5 pEC50 315 nM EC50 Bioorg Med Chem Lett (2010) 20: 6797-6801 [PMID:20851601]
ChEMBL Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay F 6.91 pEC50 123 nM EC50 Bioorg Med Chem Lett (2012) 22: 2943-2947 [PMID:22424974]
ChEMBL Agonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis F 7.38 pEC50 41.69 nM EC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis F 8.74 pEC50 1.8 nM EC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis F 8.82 pEC50 1.51 nM EC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Agonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis F 8.86 pEC50 1.38 nM EC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Agonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis F 9.28 pEC50 0.52 nM EC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
CCK1 receptor/Cholecystokinin A receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551]
ChEMBL Displacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counter B 7.12 pIC50 76.54 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells B 7.91 pIC50 12.2 nM IC50 Bioorg Med Chem Lett (2010) 20: 6797-6801 [PMID:20851601]
ChEMBL Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay F 6.35 pEC50 445.8 nM EC50 Bioorg Med Chem Lett (2010) 20: 6797-6801 [PMID:20851601]
CCK2 receptor/Cholecystokinin B receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239]
ChEMBL Displacement of [125I-CCK] from wild-type human CCK2R expressed in CHO cells after 60 mins by scintillation counter B 6 pKi >1000 nM Ki J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-2] from wild-type human CCK2R expressed in CHO cells after 60 mins by scintillation counter B 6.77 pKi 169.82 nM Ki J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-CCK] from wild-type human CCK2R at allosteric site expressed in CHO cells after 60 mins by scintillation counter B 7.15 pKi 70.79 nM Ki J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-2] from wild-type human CCK2R at allosteric site expressed in CHO cells after 60 mins by scintillation counter B 7.61 pKi 24.55 nM Ki J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-CCK] from human CCK2R T2.61N mutant expressed in CHO cells after 60 mins by scintillation counter B 6 pIC50 >1000 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-CCK] from human CCK2R V6.51I, Y6.52F mutant expressed in CHO cells after 60 mins by scintillation counter B 6 pIC50 >1000 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-2] from human CCK2R V3.28T, S3.29T mutant expressed in CHO cells after 60 mins by scintillation counter B 6 pIC50 >1000 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-2] from human CCK2R V6.51I, Y6.52F mutant expressed in CHO cells after 60 mins by scintillation counter B 6 pIC50 >1000 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-CCK] from wild-type human CCK2R expressed in CHO cells after 60 mins by scintillation counter B 6.56 pIC50 275.42 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-CCK] from human CCK2R V3.28T, S3.29T mutant expressed in CHO cells after 60 mins by scintillation counter B 6.68 pIC50 208.93 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-2] from wild-type human CCK2R expressed in CHO cells after 60 mins by scintillation counter B 6.76 pIC50 175 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-2] from wild-type human CCK2R expressed in CHO cells after 60 mins by scintillation counter B 6.85 pIC50 141.25 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-BDZ-2] from human CCK2R H7.39L mutant expressed in CHO cells after 60 mins by scintillation counter B 8.7 pIC50 2 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Displacement of [125I-CCK] from human CCK2R H7.39L mutant expressed in CHO cells after 60 mins by scintillation counter B 8.77 pIC50 1.7 nM IC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Partial agonist activity at wild-type human CCK2R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis F 6 pEC50 1000 nM EC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Agonist activity at human CCK2R T2.61N mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis F 6 pEC50 >1000 nM EC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Agonist activity at human CCK2R V3.28T, S3.29T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis F 6 pEC50 >1000 nM EC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Partial agonist activity at wild-type human CCK2R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis F 6.01 pEC50 977.24 nM EC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Agonist activity at human CCK2R V6.51I, Y6.52F mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis F 6.55 pEC50 281.84 nM EC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]
ChEMBL Agonist activity at human CCK2R H7.39L mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis F 7.23 pEC50 58.88 nM EC50 J Med Chem (2015) 58: 9562-9577 [PMID:26654202]

ChEMBL data shown on this page come from version 34:

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]