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) |
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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 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]
