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Assay Detail

CHEMBL909349

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

Binding
Inhibition of tetramethylrhodamine labeled dexamethasone binding to GR by FP assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
Regan J, Lee TW, Zindell RM, Bekkali Y, Bentzien J, Gilmore T, Hammach A, Kirrane TM, Kukulka AJ, Kuzmich D, Nelson RM, Proudfoot JR, Ralph M, Pelletier J, Souza D, Zuvela-Jelaska L, Nabozny G, Thomson DS.
J Med Chem (2006) 49 : 7887 -7896
PubMed 17181172 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.52 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL216272 1 8.52
CHEMBL219207 1 8.52
CHEMBL384467 DEXAMETHASONE 4.0 1 8.52
CHEMBL373497 1 8.40
CHEMBL219314 1 8.40
CHEMBL219973 1 8.30
CHEMBL375838 1 8.22
CHEMBL263091 1 8.10
CHEMBL384081 1 8.10
CHEMBL216273 1 8.00
CHEMBL216173 1 8.00
CHEMBL386465 1 8.00
CHEMBL219561 1 7.96
CHEMBL131 PREDNISOLONE 4.0 1 7.82
CHEMBL386915 1 7.82
CHEMBL425970 1 7.66
CHEMBL219069 1 7.55
CHEMBL386916 1 7.47
CHEMBL219084 1 7.47
CHEMBL375348 1 7.42
CHEMBL374327 1 7.32
CHEMBL373498 1 7.27
CHEMBL219140 1 7.11
CHEMBL218830 1 6.96
CHEMBL219015 1 6.92
CHEMBL219016 1 6.90
CHEMBL220023 1 6.19
CHEMBL219068 1 6.16
CHEMBL373567 1 6.11
CHEMBL218976 1 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL216272 IC50 = 3.0 nM 8.52
CHEMBL384467 DEXAMETHASONE IC50 = 3.0 nM 8.52
CHEMBL219207 IC50 = 3.0 nM 8.52
CHEMBL373497 IC50 = 4.0 nM 8.40
CHEMBL219314 IC50 = 4.0 nM 8.40
CHEMBL219973 IC50 = 5.0 nM 8.30
CHEMBL375838 IC50 = 6.0 nM 8.22
CHEMBL263091 IC50 = 8.0 nM 8.10
CHEMBL384081 IC50 = 8.0 nM 8.10
CHEMBL216273 IC50 = 10.0 nM 8.00
CHEMBL216173 IC50 = 10.0 nM 8.00
CHEMBL386465 IC50 = 10.0 nM 8.00
CHEMBL219561 IC50 = 11.0 nM 7.96
CHEMBL131 PREDNISOLONE IC50 = 15.0 nM 7.82
CHEMBL386915 IC50 = 15.0 nM 7.82
CHEMBL425970 IC50 = 22.0 nM 7.66
CHEMBL219069 IC50 = 28.0 nM 7.55
CHEMBL386916 IC50 = 34.0 nM 7.47
CHEMBL219084 IC50 = 34.0 nM 7.47
CHEMBL375348 IC50 = 38.0 nM 7.42
CHEMBL374327 IC50 = 48.0 nM 7.32
CHEMBL373498 IC50 = 54.0 nM 7.27
CHEMBL219140 IC50 = 77.0 nM 7.11
CHEMBL218830 IC50 = 110.0 nM 6.96
CHEMBL219015 IC50 = 120.0 nM 6.92
CHEMBL219016 IC50 = 125.0 nM 6.90
CHEMBL220023 IC50 = 650.0 nM 6.19
CHEMBL219068 IC50 = 690.0 nM 6.16
CHEMBL373567 IC50 = 780.0 nM 6.11
CHEMBL218976 IC50 = 950.0 nM 6.02
CHEMBL218778 IC50 = 1400.0 nM 5.85
CHEMBL219205 IC50 > 2000.0 nM -
CHEMBL435753 IC50 > 2000.0 nM -
CHEMBL219290 IC50 > 2000.0 nM -