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Assay Detail

CHEMBL976505

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Functional
Agonist activity at human CCK1 receptor
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 26 9.95 10.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL504406 1 10.48
CHEMBL498958 1 10.47
CHEMBL502974 1 10.40
CHEMBL509464 1 10.28
CHEMBL504861 1 10.26
CHEMBL468372 1 10.19
CHEMBL504114 1 10.15
CHEMBL507094 1 10.13
CHEMBL503107 1 10.09
CHEMBL450105 1 10.05
CHEMBL505727 1 10.03
CHEMBL446324 1 10.02
CHEMBL508004 1 10.01
CHEMBL503331 1 10.01
CHEMBL508772 1 10.01
CHEMBL451342 1 10.00
CHEMBL450443 1 10.00
CHEMBL507051 1 9.89
CHEMBL505432 1 9.85
CHEMBL446502 1 9.80
CHEMBL449681 1 9.74
CHEMBL449725 1 9.68
CHEMBL502924 1 9.60
CHEMBL448118 1 9.34
CHEMBL453083 1 9.14
CHEMBL504707 1 9.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL504406 EC50 = 0.033 nM 10.48
CHEMBL498958 EC50 = 0.034 nM 10.47
CHEMBL502974 EC50 = 0.04 nM 10.40
CHEMBL509464 EC50 = 0.053 nM 10.28
CHEMBL504861 EC50 = 0.055 nM 10.26
CHEMBL468372 EC50 = 0.065 nM 10.19
CHEMBL504114 EC50 = 0.071 nM 10.15
CHEMBL507094 EC50 = 0.074 nM 10.13
CHEMBL503107 EC50 = 0.082 nM 10.09
CHEMBL450105 EC50 = 0.089 nM 10.05
CHEMBL505727 EC50 = 0.094 nM 10.03
CHEMBL446324 EC50 = 0.095 nM 10.02
CHEMBL508004 EC50 = 0.097 nM 10.01
CHEMBL503331 EC50 = 0.097 nM 10.01
CHEMBL508772 EC50 = 0.097 nM 10.01
CHEMBL451342 EC50 = 0.1 nM 10.00
CHEMBL450443 EC50 = 0.1 nM 10.00
CHEMBL507051 EC50 = 0.13 nM 9.89
CHEMBL505432 EC50 = 0.14 nM 9.85
CHEMBL446502 EC50 = 0.16 nM 9.80
CHEMBL449681 EC50 = 0.18 nM 9.74
CHEMBL449725 EC50 = 0.21 nM 9.68
CHEMBL502924 EC50 = 0.25 nM 9.60
CHEMBL448118 EC50 = 0.46 nM 9.34
CHEMBL453083 EC50 = 0.73 nM 9.14
CHEMBL504707 EC50 = 0.77 nM 9.11