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Assay Detail

CHEMBL916640

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

Binding
Displacement of radiolabeled Dexamethasone from human GR
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
Higuchi RI, Arienti KL, López FJ, Mani NS, Mais DE, Caferro TR, Long YO, Jones TK, Edwards JP, Zhi L, Schrader WT, Negro-Vilar A, Marschke KB.
J Med Chem (2007) 50 : 2486 -2496
PubMed 17439112 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.09 5.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388997 1 5.19
CHEMBL224204 1 5.09
CHEMBL227440 1 5.07
CHEMBL227784 1 5.06
CHEMBL227783 1 5.04
CHEMBL226609 1 -
CHEMBL389481 1 -
CHEMBL227408 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388997 Ki = 6500.0 nM 5.19
CHEMBL224204 Ki = 8100.0 nM 5.09
CHEMBL227440 Ki = 8500.0 nM 5.07
CHEMBL227784 Ki = 8800.0 nM 5.06
CHEMBL227783 Ki = 9200.0 nM 5.04
CHEMBL226609 Ki > 10000.0 nM -
CHEMBL389481 Ki > 10000.0 nM -
CHEMBL227408 Ki > 10000.0 nM -