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Assay Detail

CHEMBL2025282

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Binding
Transrepression activity at glucocorticoid receptor in human H292 cells assessed as inhibition of TNF-induced IL8 production
ChEMBL ↗
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type H292
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glucocorticoid receptor (CHEMBL2034) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Steroidal C-21 heteroaryl thioethers. Part 3: pregn-4-eno-[3,2-c]pyrazole fused A ring modified steroids as selective glucocorticoid receptor modulators (dissociated steroids).
Biju P, Wang H, Anthes J, McCormick K, Aslanian R, Berlin M, Bitar R, Lim YH, Lee YJ, Prelusky D, Mcleod R, Jia Y, Fernandez X, Lieber G, Jimenez J, Eckel S, House A, Chapman R, Phillips J.
Bioorg Med Chem Lett (2012) 22 : 3291 -3295
PubMed 22465636 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 8.20 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2023619 — — 1 9.49
CHEMBL2022858 — — 1 9.40
CHEMBL2021945 — — 1 9.30
CHEMBL2023620 — — 1 9.22
CHEMBL2022651 — — 1 9.20
CHEMBL2023243 — — 1 9.14
CHEMBL2022656 — — 1 9.05
CHEMBL2023244 — — 1 8.97
CHEMBL2023241 — — 1 8.96
CHEMBL2022657 — — 1 8.82
CHEMBL2023618 — — 1 8.80
CHEMBL2023239 — — 1 8.77
CHEMBL2023615 — — 1 8.74
CHEMBL2023617 — — 1 8.72
CHEMBL2023616 — — 1 8.70
CHEMBL2023240 — — 1 8.68
CHEMBL2022652 — — 1 8.62
CHEMBL2022865 — — 1 8.55
CHEMBL2023242 — — 1 8.54
CHEMBL2023621 — — 1 8.52
CHEMBL2022655 — — 1 8.51
CHEMBL2022866 — — 1 8.46
CHEMBL2022864 — — 1 8.43
CHEMBL2022658 — — 1 8.36
CHEMBL2022653 — — 1 8.33
CHEMBL2023614 — — 1 8.28
CHEMBL2022862 — — 1 8.27
CHEMBL2022654 — — 1 8.18
CHEMBL2023236 — — 1 8.15
CHEMBL2022659 — — 1 8.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2023619 — IC50 = 0.32 nM 9.49
CHEMBL2022858 — IC50 = 0.4 nM 9.40
CHEMBL2021945 — IC50 = 0.5 nM 9.30
CHEMBL2023620 — IC50 = 0.6 nM 9.22
CHEMBL2022651 — IC50 = 0.63 nM 9.20
CHEMBL2023243 — IC50 = 0.72 nM 9.14
CHEMBL2022656 — IC50 = 0.89 nM 9.05
CHEMBL2023244 — IC50 = 1.06 nM 8.97
CHEMBL2023241 — IC50 = 1.1 nM 8.96
CHEMBL2022657 — IC50 = 1.5 nM 8.82
CHEMBL2023618 — IC50 = 1.6 nM 8.80
CHEMBL2023239 — IC50 = 1.7 nM 8.77
CHEMBL2023615 — IC50 = 1.8 nM 8.74
CHEMBL2023617 — IC50 = 1.89 nM 8.72
CHEMBL2023616 — IC50 = 1.99 nM 8.70
CHEMBL2023240 — IC50 = 2.1 nM 8.68
CHEMBL2022652 — IC50 = 2.37 nM 8.62
CHEMBL2022865 — IC50 = 2.8 nM 8.55
CHEMBL2023242 — IC50 = 2.9 nM 8.54
CHEMBL2023621 — IC50 = 3.0 nM 8.52
CHEMBL2022655 — IC50 = 3.12 nM 8.51
CHEMBL2022866 — IC50 = 3.43 nM 8.46
CHEMBL2022864 — IC50 = 3.7 nM 8.43
CHEMBL2022658 — IC50 = 4.4 nM 8.36
CHEMBL2022653 — IC50 = 4.7 nM 8.33
CHEMBL2023614 — IC50 = 5.3 nM 8.28
CHEMBL2022862 — IC50 = 5.36 nM 8.27
CHEMBL2022654 — IC50 = 6.6 nM 8.18
CHEMBL2023236 — IC50 = 7.1 nM 8.15
CHEMBL2022659 — IC50 = 7.3 nM 8.14
CHEMBL2022859 — IC50 = 7.5 nM 8.12
CHEMBL2022863 — IC50 = 12.4 nM 7.91
CHEMBL2022660 — IC50 = 14.8 nM 7.83
CHEMBL2024022 — IC50 = 21.9 nM 7.66
CHEMBL2024024 — IC50 = 22.1 nM 7.66
CHEMBL2024028 — IC50 = 23.8 nM 7.62
CHEMBL2024021 — IC50 = 26.7 nM 7.57
CHEMBL2024030 — IC50 = 27.2 nM 7.57
CHEMBL2024027 — IC50 = 29.2 nM 7.54
CHEMBL1917242 — IC50 = 36.0 nM 7.44
CHEMBL2022861 — IC50 = 44.7 nM 7.35
CHEMBL2024020 — IC50 = 56.1 nM 7.25
CHEMBL2024026 — IC50 = 59.1 nM 7.23
CHEMBL2024025 — IC50 = 61.3 nM 7.21
CHEMBL2023235 — IC50 = 86.4 nM 7.06
CHEMBL2024023 — IC50 = 89.3 nM 7.05
CHEMBL2023233 — IC50 = 107.0 nM 6.97
CHEMBL2024029 — IC50 = 127.0 nM 6.90
CHEMBL2023234 — IC50 = 179.0 nM 6.75