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Assay Detail

CHEMBL863064

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

Binding
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
29
Total Activities
17
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
Agnes RS, Lee YS, Davis P, Ma SW, Badghisi H, Porreca F, Lai J, Hruby VJ.
J Med Chem (2006) 49 : 2868 -2875
PubMed 16686530 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.82 8.02
Ki 12 5.99 8.02
Log IC50 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL208479 2 8.02
CHEMBL382051 2 7.01
CHEMBL206974 2 6.50
CHEMBL408083 2 6.04
CHEMBL218327 2 5.96
CHEMBL379405 2 5.71
CHEMBL407057 2 5.50
CHEMBL218763 2 5.44
CHEMBL382349 2 5.29
CHEMBL262172 2 5.24
CHEMBL383458 2 5.19
CHEMBL205965 2 4.98
CHEMBL205306 1 -
CHEMBL1121 SINCALIDE 4.0 1 -
CHEMBL336381 1 -
CHEMBL382409 1 -
CHEMBL408330 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL208479 IC50 = 9.55 nM 8.02
CHEMBL208479 Ki = 9.6 nM 8.02
CHEMBL382051 Ki = 98.0 nM 7.01
CHEMBL382051 IC50 = 97.72 nM 7.01
CHEMBL206974 IC50 = 316.23 nM 6.50
CHEMBL206974 Ki = 320.0 nM 6.50
CHEMBL408083 Ki = 910.0 nM 6.04
CHEMBL218327 Ki = 1100.0 nM 5.96
CHEMBL218327 IC50 = 1096.48 nM 5.96
CHEMBL379405 IC50 = 1949.84 nM 5.71
CHEMBL379405 Ki = 2000.0 nM 5.70
CHEMBL407057 Ki = 3200.0 nM 5.50
CHEMBL407057 IC50 = 3162.28 nM 5.50
CHEMBL218763 IC50 = 3630.78 nM 5.44
CHEMBL218763 Ki = 3600.0 nM 5.44
CHEMBL382349 IC50 = 5128.61 nM 5.29
CHEMBL382349 Ki = 5100.0 nM 5.29
CHEMBL262172 IC50 = 5754.4 nM 5.24
CHEMBL262172 Ki = 5700.0 nM 5.24
CHEMBL383458 Ki = 6500.0 nM 5.19
CHEMBL383458 IC50 = 6456.54 nM 5.19
CHEMBL408083 IC50 = 9120.11 nM 5.04
CHEMBL205965 IC50 = 10471.29 nM 4.98
CHEMBL205306 Log IC50 - -
CHEMBL1121 SINCALIDE Log IC50 - -
CHEMBL336381 Log IC50 - -
CHEMBL382409 Log IC50 - -
CHEMBL205965 Ki > 10000.0 nM -
CHEMBL408330 Log IC50 - -