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Assay Detail

CHEMBL909387

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

Binding
Displacement of [125I]CCK8-SO3 from human CCK2 receptor expressed in HEK293 cells
14
Total Activities
7
Compounds Tested
2
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

Gastrin/cholecystokinin type B receptor (CHEMBL298)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
Lee YS, Agnes RS, Davis P, Ma SW, Badghisi H, Lai J, Porreca F, Hruby VJ.
J Med Chem (2007) 50 : 165 -168
PubMed 17201419 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.46 6.77
Ki 7 5.81 7.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL217957 2 7.15
CHEMBL218600 2 5.96
CHEMBL386212 2 5.11
CHEMBL407198 2 5.03
CHEMBL414087 2 5.00
CHEMBL218651 2 4.87
CHEMBL386186 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL217957 Ki = 71.0 nM 7.15
CHEMBL217957 IC50 = 169.82 nM 6.77
CHEMBL218600 IC50 = 1096.48 nM 5.96
CHEMBL218600 Ki = 1100.0 nM 5.96
CHEMBL386212 IC50 = 7762.47 nM 5.11
CHEMBL386212 Ki = 7700.0 nM 5.11
CHEMBL407198 IC50 = 9332.54 nM 5.03
CHEMBL407198 Ki = 9300.0 nM 5.03
CHEMBL414087 IC50 = 10000.0 nM 5.00
CHEMBL218651 IC50 = 13489.63 nM 4.87
CHEMBL414087 Ki > 10000.0 nM -
CHEMBL386186 IC50 = 66069344.8 nM -
CHEMBL386186 Ki > 10000.0 nM -
CHEMBL218651 Ki > 10000.0 nM -