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Assay Detail

CHEMBL994440

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Binding
Inhibition of human CCK1 receptor
ChEMBL ↗
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholecystokinin receptor type A (CHEMBL1901) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of imidazole carboxamides as potent and selective CCK1R agonists.
Zhu C, Hansen AR, Bateman T, Chen Z, Holt TG, Hubert JA, Karanam BV, Lee SJ, Pan J, Qian S, Reddy VB, Reitman ML, Strack AM, Tong V, Weingarth DT, Wolff MS, MacNeil DJ, Weber AE, Duffy JL, Edmondson SD.
Bioorg Med Chem Lett (2008) 18 : 4393 -4396
PubMed 18614364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 8.56 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL505225 — — 1 10.52
CHEMBL509519 — — 1 10.52
CHEMBL504861 — — 1 10.22
CHEMBL510690 — — 1 10.15
CHEMBL498942 — — 1 10.10
CHEMBL505727 — — 1 9.92
CHEMBL475679 — — 1 9.92
CHEMBL451644 — — 1 9.85
CHEMBL448221 — — 1 9.85
CHEMBL514953 — — 1 9.70
CHEMBL474067 — — 1 9.62
CHEMBL478398 — — 1 9.38
CHEMBL453083 — — 1 9.35
CHEMBL473664 — — 1 9.25
CHEMBL515887 — — 1 9.24
CHEMBL473865 — — 1 9.22
CHEMBL473663 — — 1 9.00
CHEMBL479256 — — 1 8.89
CHEMBL455742 — — 1 8.89
CHEMBL473457 — — 1 8.72
CHEMBL516355 — — 1 8.72
CHEMBL515161 — — 1 8.72
CHEMBL476530 — — 1 8.72
CHEMBL515616 — — 1 8.64
CHEMBL479046 — — 1 8.60
CHEMBL476520 — — 1 8.47
CHEMBL476531 — — 1 8.25
CHEMBL516113 — — 1 8.16
CHEMBL476095 — — 1 8.10
CHEMBL478630 — — 1 8.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL505225 — IC50 = 0.03 nM 10.52
CHEMBL509519 — IC50 = 0.03 nM 10.52
CHEMBL504861 — IC50 = 0.06 nM 10.22
CHEMBL510690 — IC50 = 0.07 nM 10.15
CHEMBL498942 — IC50 = 0.08 nM 10.10
CHEMBL505727 — IC50 = 0.12 nM 9.92
CHEMBL475679 — IC50 = 0.12 nM 9.92
CHEMBL451644 — IC50 = 0.14 nM 9.85
CHEMBL448221 — IC50 = 0.14 nM 9.85
CHEMBL514953 — IC50 = 0.2 nM 9.70
CHEMBL474067 — IC50 = 0.24 nM 9.62
CHEMBL478398 — IC50 = 0.42 nM 9.38
CHEMBL453083 — IC50 = 0.45 nM 9.35
CHEMBL473664 — IC50 = 0.56 nM 9.25
CHEMBL515887 — IC50 = 0.57 nM 9.24
CHEMBL473865 — IC50 = 0.6 nM 9.22
CHEMBL473663 — IC50 = 1.0 nM 9.00
CHEMBL479256 — IC50 = 1.3 nM 8.89
CHEMBL455742 — IC50 = 1.3 nM 8.89
CHEMBL476530 — IC50 = 1.9 nM 8.72
CHEMBL515161 — IC50 = 1.9 nM 8.72
CHEMBL473457 — IC50 = 1.9 nM 8.72
CHEMBL516355 — IC50 = 1.9 nM 8.72
CHEMBL515616 — IC50 = 2.3 nM 8.64
CHEMBL479046 — IC50 = 2.5 nM 8.60
CHEMBL476520 — IC50 = 3.4 nM 8.47
CHEMBL476531 — IC50 = 5.6 nM 8.25
CHEMBL516113 — IC50 = 6.9 nM 8.16
CHEMBL476095 — IC50 = 8.0 nM 8.10
CHEMBL478630 — IC50 = 8.6 nM 8.07
CHEMBL478604 — IC50 = 14.0 nM 7.85
CHEMBL476739 — IC50 = 16.0 nM 7.80
CHEMBL477996 — IC50 = 17.0 nM 7.77
CHEMBL476297 — IC50 = 22.0 nM 7.66
CHEMBL478397 — IC50 = 30.0 nM 7.52
CHEMBL515160 — IC50 = 35.0 nM 7.46
CHEMBL479063 — IC50 = 41.0 nM 7.39
CHEMBL476725 — IC50 = 43.0 nM 7.37
CHEMBL476747 — IC50 = 43.0 nM 7.37
CHEMBL504024 — IC50 = 130.0 nM 6.89
CHEMBL476519 — IC50 = 140.0 nM 6.85
CHEMBL479030 — IC50 = 160.0 nM 6.80
CHEMBL514716 — IC50 = 190.0 nM 6.72
CHEMBL448597 — IC50 = 200.0 nM 6.70
CHEMBL477784 — IC50 = 630.0 nM 6.20