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Assay Detail

CHEMBL909397

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Functional
Activity at human CCK2 receptor expressed in HEK293 cells assessed as level of [3H]inositol produced relative to control
9
Total Activities
3
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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 3 7.90 8.34
EC50 3 7.90 8.34
Emax 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL407198 3 8.34
CHEMBL414087 3 7.80
CHEMBL375360 3 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL407198 IC50 = 4.571 nM 8.34
CHEMBL407198 EC50 = 4.6 nM 8.34
CHEMBL414087 IC50 = 15.85 nM 7.80
CHEMBL414087 EC50 = 16.0 nM 7.80
CHEMBL375360 IC50 = 26.92 nM 7.57
CHEMBL375360 EC50 = 27.0 nM 7.57
CHEMBL414087 Emax = 11.0 -
CHEMBL375360 Emax = 16.0 -
CHEMBL407198 Emax = 22.0 -