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Assay Detail

CHEMBL694626

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

Functional
Effective concentration in HepG2 cells transfected with LUC gene (E-sel-Luc).
26
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HepG2
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Nonsteroidal selective glucocorticoid modulators: the effect of C-5 alkyl substitution on the transcriptional activation/repression profile of 2,5-dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.
Elmore SW, Coghlan MJ, Anderson DD, Pratt JK, Green BE, Wang AX, Stashko MA, Lin CW, Tyree CM, Miner JN, Jacobson PB, Wilcox DM, Lane BC.
J Med Chem (2001) 44 : 4481 -4491
PubMed 11728194 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 26 7.31 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL131 PREDNISOLONE 4.0 1 8.59
CHEMBL97206 1 8.40
CHEMBL266282 AL-43 3 8.16
CHEMBL141836 1 7.82
CHEMBL337112 1 7.75
CHEMBL141915 1 7.66
CHEMBL138098 1 7.57
CHEMBL141282 1 7.41
CHEMBL137982 1 7.16
CHEMBL336041 1 7.16
CHEMBL141344 1 7.05
CHEMBL140336 1 6.91
CHEMBL138003 1 6.90
CHEMBL137890 1 6.84
CHEMBL138197 1 6.78
CHEMBL141524 1 6.69
CHEMBL343135 1 6.59
CHEMBL141426 1 6.51
CHEMBL138957 1 -
CHEMBL138737 1 -
CHEMBL141361 1 -
CHEMBL138753 1 -
CHEMBL140553 1 -
CHEMBL342819 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL131 PREDNISOLONE EC50 = 2.6 nM 8.59
CHEMBL97206 EC50 = 4.0 nM 8.40
CHEMBL266282 AL-43 EC50 = 6.9 nM 8.16
CHEMBL266282 AL-43 EC50 = 13.0 nM 7.89
CHEMBL141836 EC50 = 15.0 nM 7.82
CHEMBL337112 EC50 = 18.0 nM 7.75
CHEMBL141915 EC50 = 22.0 nM 7.66
CHEMBL138098 EC50 = 27.0 nM 7.57
CHEMBL141282 EC50 = 39.0 nM 7.41
CHEMBL137982 EC50 = 69.0 nM 7.16
CHEMBL336041 EC50 = 70.0 nM 7.16
CHEMBL141344 EC50 = 90.0 nM 7.05
CHEMBL140336 EC50 = 122.0 nM 6.91
CHEMBL138003 EC50 = 126.0 nM 6.90
CHEMBL137890 EC50 = 144.0 nM 6.84
CHEMBL138197 EC50 = 168.0 nM 6.78
CHEMBL141524 EC50 = 204.0 nM 6.69
CHEMBL343135 EC50 = 255.0 nM 6.59
CHEMBL141426 EC50 = 306.0 nM 6.51
CHEMBL266282 AL-43 EC50 = 450.0 nM 6.35
CHEMBL138737 EC50 > 5000.0 nM -
CHEMBL138957 EC50 > 5000.0 nM -
CHEMBL141361 EC50 > 5000.0 nM -
CHEMBL138753 EC50 > 5000.0 nM -
CHEMBL140553 EC50 > 5000.0 nM -
CHEMBL342819 EC50 > 5000.0 nM -