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Assay Detail

CHEMBL976507

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Binding
Inhibition of human CCK1 receptor
26
Total Activities
26
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

2-Substituted piperazine-derived imidazole carboxamides as potent and selective CCK1R agonists for the treatment of obesity.
Berger R, Zhu C, Hansen AR, Harper B, Chen Z, Holt TG, Hubert J, Lee SJ, Pan J, Qian S, Reitman ML, Strack AM, Weingarth DT, Wolff M, Macneil DJ, Weber AE, Edmondson SD.
Bioorg Med Chem Lett (2008) 18 : 4833 -4837
PubMed 18684621 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 9.95 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL504114 1 11.00
CHEMBL509464 1 10.80
CHEMBL450105 1 10.74
CHEMBL508004 1 10.41
CHEMBL504861 1 10.40
CHEMBL498958 1 10.39
CHEMBL468372 1 10.28
CHEMBL504406 1 10.24
CHEMBL451342 1 10.17
CHEMBL502974 1 10.10
CHEMBL507051 1 10.10
CHEMBL507094 1 10.01
CHEMBL503107 1 9.96
CHEMBL505727 1 9.92
CHEMBL446324 1 9.92
CHEMBL508772 1 9.85
CHEMBL449681 1 9.68
CHEMBL502924 1 9.62
CHEMBL505432 1 9.62
CHEMBL450443 1 9.60
CHEMBL503331 1 9.41
CHEMBL449725 1 9.37
CHEMBL453083 1 9.35
CHEMBL504707 1 9.33
CHEMBL446502 1 9.25
CHEMBL448118 1 9.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL504114 IC50 = 0.01 nM 11.00
CHEMBL509464 IC50 = 0.016 nM 10.80
CHEMBL450105 IC50 = 0.018 nM 10.74
CHEMBL508004 IC50 = 0.039 nM 10.41
CHEMBL504861 IC50 = 0.04 nM 10.40
CHEMBL498958 IC50 = 0.041 nM 10.39
CHEMBL468372 IC50 = 0.052 nM 10.28
CHEMBL504406 IC50 = 0.058 nM 10.24
CHEMBL451342 IC50 = 0.067 nM 10.17
CHEMBL502974 IC50 = 0.08 nM 10.10
CHEMBL507051 IC50 = 0.08 nM 10.10
CHEMBL507094 IC50 = 0.097 nM 10.01
CHEMBL503107 IC50 = 0.11 nM 9.96
CHEMBL505727 IC50 = 0.12 nM 9.92
CHEMBL446324 IC50 = 0.12 nM 9.92
CHEMBL508772 IC50 = 0.14 nM 9.85
CHEMBL449681 IC50 = 0.21 nM 9.68
CHEMBL502924 IC50 = 0.24 nM 9.62
CHEMBL505432 IC50 = 0.24 nM 9.62
CHEMBL450443 IC50 = 0.25 nM 9.60
CHEMBL503331 IC50 = 0.39 nM 9.41
CHEMBL449725 IC50 = 0.43 nM 9.37
CHEMBL453083 IC50 = 0.45 nM 9.35
CHEMBL504707 IC50 = 0.47 nM 9.33
CHEMBL446502 IC50 = 0.56 nM 9.25
CHEMBL448118 IC50 = 0.73 nM 9.14