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Assay Detail

CHEMBL896154

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

Functional
Agonist activity at human GR expressed in CV1 cells by GRE activation assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma.
Hudson AR, Roach SL, Higuchi RI, Phillips DP, Bissonnette RP, Lamph WW, Yen J, Li Y, Adams ME, Valdez LJ, Vassar A, Cuervo C, Kallel EA, Gharbaoui CJ, Mais DE, Miner JN, Marschke KB, Rungta D, Negro-Vilar A, Zhi L.
J Med Chem (2007) 50 : 4699 -4709
PubMed 17705362 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 9.35 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL397920 1 10.00
CHEMBL384467 DEXAMETHASONE 4.0 1 9.70
CHEMBL395717 1 9.70
CHEMBL395716 1 9.70
CHEMBL394369 1 9.70
CHEMBL243455 1 9.52
CHEMBL244714 1 9.40
CHEMBL428922 1 9.30
CHEMBL429466 1 9.30
CHEMBL244535 1 9.22
CHEMBL244715 1 8.85
CHEMBL243469 1 8.80
CHEMBL397919 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL397920 EC50 = 0.1 nM 10.00
CHEMBL384467 DEXAMETHASONE EC50 = 0.2 nM 9.70
CHEMBL395717 EC50 = 0.2 nM 9.70
CHEMBL395716 EC50 = 0.2 nM 9.70
CHEMBL394369 EC50 = 0.2 nM 9.70
CHEMBL243455 EC50 = 0.3 nM 9.52
CHEMBL244714 EC50 = 0.4 nM 9.40
CHEMBL428922 EC50 = 0.5 nM 9.30
CHEMBL429466 EC50 = 0.5 nM 9.30
CHEMBL244535 EC50 = 0.6 nM 9.22
CHEMBL244715 EC50 = 1.4 nM 8.85
CHEMBL243469 EC50 = 1.6 nM 8.80
CHEMBL397919 EC50 = 5.0 nM 8.30