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Assay Detail

CHEMBL3619503

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

Binding
Inverse agonist activity at GAL4-fused human RORc expressed in HEK293 cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nuclear receptor ROR-gamma (CHEMBL1741186)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists.
Fauber BP, Gobbi A, Savy P, Burton B, Deng Y, Everett C, La H, Johnson AR, Lockey P, Norman M, Wong H.
Bioorg Med Chem Lett (2015) 25 : 4109 -4113
PubMed 26321361 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.25 5.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3617309 1 5.48
CHEMBL3314003 1 5.41
CHEMBL3617295 1 5.18
CHEMBL3617297 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3617309 EC50 = 3300.0 nM 5.48
CHEMBL3314003 EC50 = 3900.0 nM 5.41
CHEMBL3617295 EC50 = 6600.0 nM 5.18
CHEMBL3617297 EC50 = 12000.0 nM 4.92