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Assay Detail

CHEMBL1775452

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Functional
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of pyrimidine carboxamides as potent and selective CCK1 receptor agonists.
Wang L, Hubert JA, Lee SJ, Pan J, Qian S, Reitman ML, Strack AM, Weingarth DT, MacNeil DJ, Weber AE, Edmondson SD.
Bioorg Med Chem Lett (2011) 21 : 2911 -2915
PubMed 21493064 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 7.95 10.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1774043 1 10.20
CHEMBL1773877 1 10.19
CHEMBL1774042 1 9.70
CHEMBL1774033 1 9.62
CHEMBL1774032 1 9.15
CHEMBL1773891 1 9.14
CHEMBL1773887 1 8.89
CHEMBL1773896 1 8.74
CHEMBL1773892 1 8.21
CHEMBL1774036 1 8.12
CHEMBL1774041 1 8.02
CHEMBL1774037 1 8.00
CHEMBL1774035 1 7.77
CHEMBL1773888 1 7.68
CHEMBL1774034 1 7.57
CHEMBL1773886 1 7.47
CHEMBL1773893 1 7.43
CHEMBL1773878 1 7.42
CHEMBL1774038 1 7.39
CHEMBL1773885 1 7.38
CHEMBL1774040 1 7.23
CHEMBL1773895 1 7.21
CHEMBL1773890 1 7.06
CHEMBL1773894 1 6.71
CHEMBL1773889 1 6.59
CHEMBL1773884 1 6.54
CHEMBL1774039 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1774043 EC50 = 0.063 nM 10.20
CHEMBL1773877 EC50 = 0.065 nM 10.19
CHEMBL1774042 EC50 = 0.2 nM 9.70
CHEMBL1774033 EC50 = 0.24 nM 9.62
CHEMBL1774032 EC50 = 0.71 nM 9.15
CHEMBL1773891 EC50 = 0.73 nM 9.14
CHEMBL1773887 EC50 = 1.3 nM 8.89
CHEMBL1773896 EC50 = 1.8 nM 8.74
CHEMBL1773892 EC50 = 6.1 nM 8.21
CHEMBL1774036 EC50 = 7.5 nM 8.12
CHEMBL1774041 EC50 = 9.6 nM 8.02
CHEMBL1774037 EC50 = 10.0 nM 8.00
CHEMBL1774035 EC50 = 17.0 nM 7.77
CHEMBL1773888 EC50 = 21.0 nM 7.68
CHEMBL1774034 EC50 = 27.0 nM 7.57
CHEMBL1773886 EC50 = 34.0 nM 7.47
CHEMBL1773893 EC50 = 37.0 nM 7.43
CHEMBL1773878 EC50 = 38.0 nM 7.42
CHEMBL1774038 EC50 = 41.0 nM 7.39
CHEMBL1773885 EC50 = 42.0 nM 7.38
CHEMBL1774040 EC50 = 59.0 nM 7.23
CHEMBL1773895 EC50 = 61.0 nM 7.21
CHEMBL1773890 EC50 = 88.0 nM 7.06
CHEMBL1773894 EC50 = 196.0 nM 6.71
CHEMBL1773889 EC50 = 256.0 nM 6.59
CHEMBL1773884 EC50 = 286.0 nM 6.54
CHEMBL1774039 EC50 = 5020.0 nM 5.30