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ChEMBL ligand: CHEMBL1269258 (Ce-326,597, Ce-326597, CE-326,597) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]