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Assay Detail

CHEMBL834748

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

Functional
Inhibition of corticotropin releasing factor stimulated cAMP production in rat pituitary assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Pituitary gland
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

Corticotropin releasing factor receptor (CHEMBL2111360)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Rational design, synthesis, and structure-activity relationships of aryltriazoles as novel corticotropin-releasing factor-1 receptor antagonists.
Lowe RF, Nelson J, Dang TN, Crowe PD, Pahuja A, McCarthy JR, Grigoriadis DE, Conlon P, Saunders J, Chen C, Szabo T, Chen TK, Bozigian H.
J Med Chem (2005) 48 : 1540 -1549
PubMed 15743196 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.93 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2094063 1 7.31
CHEMBL3085414 1 7.25
CHEMBL110609 1 7.05
CHEMBL3085416 1 7.04
CHEMBL2093962 1 7.04
CHEMBL2094043 1 6.92
CHEMBL2094044 1 6.92
CHEMBL3085417 1 6.62
CHEMBL3085418 1 6.62
CHEMBL3085415 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2094063 IC50 = 49.0 nM 7.31
CHEMBL3085414 IC50 = 56.0 nM 7.25
CHEMBL110609 IC50 = 90.0 nM 7.05
CHEMBL3085416 IC50 = 91.0 nM 7.04
CHEMBL2093962 IC50 = 92.0 nM 7.04
CHEMBL2094043 IC50 = 120.0 nM 6.92
CHEMBL2094044 IC50 = 120.0 nM 6.92
CHEMBL3085417 IC50 = 240.0 nM 6.62
CHEMBL3085418 IC50 = 240.0 nM 6.62
CHEMBL3085415 IC50 = 270.0 nM 6.57