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Assay Detail

CHEMBL1775460

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
IC50 32 7.78 10.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1773877 1 10.47
CHEMBL1773891 1 9.74
CHEMBL1774043 1 9.66
CHEMBL1774033 1 9.59
CHEMBL1774032 1 8.85
CHEMBL1774042 1 8.70
CHEMBL1773888 1 8.62
CHEMBL1773887 1 8.62
CHEMBL1774041 1 8.33
CHEMBL1773896 1 8.17
CHEMBL1774037 1 8.00
CHEMBL1774035 1 7.89
CHEMBL1774034 1 7.77
CHEMBL1773892 1 7.75
CHEMBL1774036 1 7.72
CHEMBL1773886 1 7.60
CHEMBL1773883 1 7.48
CHEMBL1773895 1 7.46
CHEMBL1773885 1 7.46
CHEMBL1773882 1 7.46
CHEMBL1773878 1 7.29
CHEMBL1773893 1 7.26
CHEMBL1774038 1 7.18
CHEMBL1774040 1 7.02
CHEMBL1773884 1 6.78
CHEMBL1773894 1 6.76
CHEMBL1774039 1 6.23
CHEMBL1773889 1 6.07
CHEMBL1773890 1 5.79
CHEMBL1773880 1 5.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1773877 IC50 = 0.034 nM 10.47
CHEMBL1773891 IC50 = 0.18 nM 9.74
CHEMBL1774043 IC50 = 0.22 nM 9.66
CHEMBL1774033 IC50 = 0.26 nM 9.59
CHEMBL1774032 IC50 = 1.4 nM 8.85
CHEMBL1774042 IC50 = 2.0 nM 8.70
CHEMBL1773888 IC50 = 2.4 nM 8.62
CHEMBL1773887 IC50 = 2.4 nM 8.62
CHEMBL1774041 IC50 = 4.7 nM 8.33
CHEMBL1773896 IC50 = 6.7 nM 8.17
CHEMBL1774037 IC50 = 9.9 nM 8.00
CHEMBL1774035 IC50 = 13.0 nM 7.89
CHEMBL1774034 IC50 = 16.9 nM 7.77
CHEMBL1773892 IC50 = 17.9 nM 7.75
CHEMBL1774036 IC50 = 19.0 nM 7.72
CHEMBL1773886 IC50 = 25.0 nM 7.60
CHEMBL1773883 IC50 = 33.0 nM 7.48
CHEMBL1773895 IC50 = 35.0 nM 7.46
CHEMBL1773885 IC50 = 35.0 nM 7.46
CHEMBL1773882 IC50 = 35.0 nM 7.46
CHEMBL1773878 IC50 = 51.0 nM 7.29
CHEMBL1773893 IC50 = 55.0 nM 7.26
CHEMBL1774038 IC50 = 66.0 nM 7.18
CHEMBL1774040 IC50 = 95.0 nM 7.02
CHEMBL1773884 IC50 = 165.0 nM 6.78
CHEMBL1773894 IC50 = 174.0 nM 6.76
CHEMBL1774039 IC50 = 587.0 nM 6.23
CHEMBL1773889 IC50 = 857.0 nM 6.07
CHEMBL1773890 IC50 = 1632.0 nM 5.79
CHEMBL1773880 IC50 = 2925.0 nM 5.53
CHEMBL1773879 IC50 > 10000.0 nM -
CHEMBL1773881 IC50 > 10000.0 nM -