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Assay Detail

CHEMBL659628

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

Binding
Half-maximal inhibition of [125I]-CCK-8(+) binding to cholecystokinin receptor from guinea pig brain tissue
ChEMBL ↗
132
Total Activities
132
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Cholecystokinin receptor (CHEMBL2095185) ↗
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.
Evans BE, Rittle KE, Bock MG, DiPardo RM, Freidinger RM, Whitter WL, Lundell GF, Veber DF, Anderson PS, Chang RS.
J Med Chem (1988) 31 : 2235 -2246
PubMed 2848124 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 132 5.01 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70883 — — 1 6.70
CHEMBL73522 — — 1 6.52
CHEMBL1907855 — — 1 6.52
CHEMBL1907661 — — 1 6.19
CHEMBL39263 — — 1 6.10
CHEMBL303227 — — 1 6.00
CHEMBL72526 — — 1 6.00
CHEMBL2092871 — — 1 5.96
CHEMBL1907841 — — 1 5.85
CHEMBL1907856 — — 1 5.82
CHEMBL2092869 — — 1 5.80
CHEMBL73946 — — 1 5.77
CHEMBL305951 — — 1 5.75
CHEMBL40668 — — 1 5.72
CHEMBL1907666 — — 1 5.68
CHEMBL441445 — — 1 5.64
CHEMBL1907846 — — 1 5.62
CHEMBL72428 — — 1 5.62
CHEMBL71950 — — 1 5.62
CHEMBL2114102 — — 1 5.57
CHEMBL1907852 — — 1 5.54
CHEMBL1907853 — — 1 5.54
CHEMBL72570 — — 1 5.54
CHEMBL1907848 — — 1 5.52
CHEMBL306806 — — 1 5.52
CHEMBL72546 — — 1 5.50
CHEMBL1907842 — — 1 5.48
CHEMBL73563 — — 1 5.48
CHEMBL40211 — — 1 5.47
CHEMBL1907851 — — 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70883 — IC50 = 200.0 nM 6.70
CHEMBL73522 — IC50 = 300.0 nM 6.52
CHEMBL1907855 — IC50 = 300.0 nM 6.52
CHEMBL1907661 — IC50 = 640.0 nM 6.19
CHEMBL39263 — IC50 = 800.0 nM 6.10
CHEMBL303227 — IC50 = 1000.0 nM 6.00
CHEMBL72526 — IC50 = 1000.0 nM 6.00
CHEMBL2092871 — IC50 = 1100.0 nM 5.96
CHEMBL1907841 — IC50 = 1400.0 nM 5.85
CHEMBL1907856 — IC50 = 1500.0 nM 5.82
CHEMBL2092869 — IC50 = 1600.0 nM 5.80
CHEMBL73946 — IC50 = 1700.0 nM 5.77
CHEMBL305951 — IC50 = 1800.0 nM 5.75
CHEMBL40668 — IC50 = 1900.0 nM 5.72
CHEMBL1907666 — IC50 = 2100.0 nM 5.68
CHEMBL441445 — IC50 = 2300.0 nM 5.64
CHEMBL71950 — IC50 = 2400.0 nM 5.62
CHEMBL1907846 — IC50 = 2400.0 nM 5.62
CHEMBL72428 — IC50 = 2400.0 nM 5.62
CHEMBL2114102 — IC50 = 2700.0 nM 5.57
CHEMBL72570 — IC50 = 2900.0 nM 5.54
CHEMBL1907852 — IC50 = 2900.0 nM 5.54
CHEMBL1907853 — IC50 = 2900.0 nM 5.54
CHEMBL1907848 — IC50 = 3000.0 nM 5.52
CHEMBL306806 — IC50 = 3000.0 nM 5.52
CHEMBL72546 — IC50 = 3200.0 nM 5.50
CHEMBL1907842 — IC50 = 3300.0 nM 5.48
CHEMBL73563 — IC50 = 3300.0 nM 5.48
CHEMBL40211 — IC50 = 3400.0 nM 5.47
CHEMBL1907851 — IC50 = 3500.0 nM 5.46
CHEMBL70593 — IC50 = 3700.0 nM 5.43
CHEMBL419764 — IC50 = 3700.0 nM 5.43
CHEMBL1907845 — IC50 = 3800.0 nM 5.42
CHEMBL1907850 — IC50 = 4000.0 nM 5.40
CHEMBL2092865 — IC50 = 4600.0 nM 5.34
CHEMBL443009 — IC50 = 5500.0 nM 5.26
CHEMBL307661 — IC50 = 5600.0 nM 5.25
CHEMBL2092866 — IC50 = 5900.0 nM 5.23
CHEMBL70456 — IC50 = 6000.0 nM 5.22
CHEMBL73885 — IC50 = 7000.0 nM 5.16
CHEMBL306760 — IC50 = 8000.0 nM 5.10
CHEMBL1907849 — IC50 = 8000.0 nM 5.10
CHEMBL74170 — IC50 = 8000.0 nM 5.10
CHEMBL307370 — IC50 = 8400.0 nM 5.08
CHEMBL2092868 — IC50 = 11000.0 nM 4.96
CHEMBL422411 — IC50 = 11000.0 nM 4.96
CHEMBL309017 — IC50 = 12000.0 nM 4.92
CHEMBL308111 — IC50 = 12000.0 nM 4.92
CHEMBL308769 — IC50 = 12000.0 nM 4.92
CHEMBL422951 — IC50 = 12000.0 nM 4.92