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Assay Detail

CHEMBL1909150

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

Binding
DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HeLa S3
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

DrugMatrix in vitro pharmacology data
Scott S. Auerbach, DrugMatrix¨ and ToxFX¨ Coordinator National Toxicology Program

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 871 6.97 8.84
Ki 871 7.31 9.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1159650 CLOBETASOL PROPIONATE 4.0 2 9.18
CHEMBL1200845 HALCINONIDE 4.0 2 9.13
CHEMBL1276308 MIFEPRISTONE 4.0 2 8.99
CHEMBL1766 DESOXIMETASONE 4.0 2 8.93
CHEMBL989 FLUOCINOLONE ACETONIDE 4.0 2 8.85
CHEMBL1200600 FLUOROMETHOLONE 4.0 2 8.80
CHEMBL1504 TRIAMCINOLONE ACETONIDE 4.0 2 8.70
CHEMBL1370 BUDESONIDE 4.0 2 8.69
CHEMBL1201012 FLURANDRENOLIDE 4.0 2 8.69
CHEMBL1501 FLUOCINONIDE 4.0 2 8.62
CHEMBL1512 FLUNISOLIDE 4.0 2 8.62
CHEMBL1200545 DIFLORASONE DIACETATE 4.0 2 8.54
CHEMBL632 BETAMETHASONE 4.0 2 8.45
CHEMBL384467 DEXAMETHASONE 4.0 2 8.44
CHEMBL1201207 BETAMETHASONE PHOSPHORIC ACID 4.0 2 8.43
CHEMBL1586 BECLOMETHASONE 2.0 2 8.43
CHEMBL650 METHYLPREDNISOLONE 4.0 2 8.30
CHEMBL131 PREDNISOLONE 4.0 2 8.13
CHEMBL1390 2 8.07
CHEMBL1201139 MEGESTROL ACETATE 4.0 2 8.06
CHEMBL717 MEDROXYPROGESTERONE ACETATE 4.0 2 8.06
CHEMBL1201010 FLUDROCORTISONE ACETATE 4.0 2 8.03
CHEMBL389621 HYDROCORTISONE 4.0 2 7.92
CHEMBL110691 CHLORMADINONE ACETATE 4.0 2 7.76
CHEMBL1062 HYDROXYPROGESTERONE 2 7.64
CHEMBL1451 TRIAMCINOLONE 4.0 2 7.58
CHEMBL2107797 NORGESTREL 4.0 2 7.17
CHEMBL241694 ETHISTERONE 3.0 2 7.02
CHEMBL139835 CYPROTERONE ACETATE 3.0 2 6.99
CHEMBL103 PROGESTERONE 4.0 2 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1159650 CLOBETASOL PROPIONATE Ki = 0.662 nM 9.18
CHEMBL1200845 HALCINONIDE Ki = 0.732 nM 9.13
CHEMBL1276308 MIFEPRISTONE Ki = 1.014 nM 8.99
CHEMBL1766 DESOXIMETASONE Ki = 1.169 nM 8.93
CHEMBL989 FLUOCINOLONE ACETONIDE Ki = 1.423 nM 8.85
CHEMBL1159650 CLOBETASOL PROPIONATE IC50 = 1.456 nM 8.84
CHEMBL1200600 FLUOROMETHOLONE Ki = 1.578 nM 8.80
CHEMBL1200845 HALCINONIDE IC50 = 1.611 nM 8.79
CHEMBL1504 TRIAMCINOLONE ACETONIDE Ki = 2.006 nM 8.70
CHEMBL1201012 FLURANDRENOLIDE Ki = 2.021 nM 8.69
CHEMBL1370 BUDESONIDE Ki = 2.034 nM 8.69
CHEMBL1276308 MIFEPRISTONE IC50 = 2.232 nM 8.65
CHEMBL1512 FLUNISOLIDE Ki = 2.423 nM 8.62
CHEMBL1501 FLUOCINONIDE Ki = 2.392 nM 8.62
CHEMBL1766 DESOXIMETASONE IC50 = 2.573 nM 8.59
CHEMBL1200545 DIFLORASONE DIACETATE Ki = 2.907 nM 8.54
CHEMBL989 FLUOCINOLONE ACETONIDE IC50 = 3.131 nM 8.50
CHEMBL1200600 FLUOROMETHOLONE IC50 = 3.471 nM 8.46
CHEMBL632 BETAMETHASONE Ki = 3.516 nM 8.45
CHEMBL384467 DEXAMETHASONE Ki = 3.664 nM 8.44
CHEMBL1586 BECLOMETHASONE Ki = 3.743 nM 8.43
CHEMBL1201207 BETAMETHASONE PHOSPHORIC ACID Ki = 3.734 nM 8.43
CHEMBL1504 TRIAMCINOLONE ACETONIDE IC50 = 4.414 nM 8.36
CHEMBL1370 BUDESONIDE IC50 = 4.475 nM 8.35
CHEMBL1201012 FLURANDRENOLIDE IC50 = 4.447 nM 8.35
CHEMBL650 METHYLPREDNISOLONE Ki = 5.033 nM 8.30
CHEMBL1501 FLUOCINONIDE IC50 = 5.263 nM 8.28
CHEMBL1512 FLUNISOLIDE IC50 = 5.33 nM 8.27
CHEMBL1200545 DIFLORASONE DIACETATE IC50 = 6.396 nM 8.19
CHEMBL131 PREDNISOLONE Ki = 7.397 nM 8.13
CHEMBL632 BETAMETHASONE IC50 = 7.735 nM 8.11
CHEMBL384467 DEXAMETHASONE IC50 = 8.06 nM 8.09
CHEMBL1201207 BETAMETHASONE PHOSPHORIC ACID IC50 = 8.216 nM 8.09
CHEMBL1586 BECLOMETHASONE IC50 = 8.234 nM 8.08
CHEMBL1390 Ki = 8.597 nM 8.07
CHEMBL1201139 MEGESTROL ACETATE Ki = 8.769 nM 8.06
CHEMBL717 MEDROXYPROGESTERONE ACETATE Ki = 8.637 nM 8.06
CHEMBL1201010 FLUDROCORTISONE ACETATE Ki = 9.253 nM 8.03
CHEMBL650 METHYLPREDNISOLONE IC50 = 11.0 nM 7.96
CHEMBL389621 HYDROCORTISONE Ki = 12.0 nM 7.92
CHEMBL131 PREDNISOLONE IC50 = 16.0 nM 7.80
CHEMBL110691 CHLORMADINONE ACETATE Ki = 17.2 nM 7.76
CHEMBL1201139 MEGESTROL ACETATE IC50 = 19.0 nM 7.72
CHEMBL1390 IC50 = 19.0 nM 7.72
CHEMBL717 MEDROXYPROGESTERONE ACETATE IC50 = 19.0 nM 7.72
CHEMBL1201010 FLUDROCORTISONE ACETATE IC50 = 20.0 nM 7.70
CHEMBL1062 HYDROXYPROGESTERONE Ki = 23.0 nM 7.64
CHEMBL389621 HYDROCORTISONE IC50 = 26.0 nM 7.58
CHEMBL1451 TRIAMCINOLONE Ki = 26.0 nM 7.58
CHEMBL110691 CHLORMADINONE ACETATE IC50 = 37.7 nM 7.42