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Assay Detail

CHEMBL4414331

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

Binding
Activation of human Gal4-fused RXRalpha LBD transfected in HEK293T after 14 to 16 hrs by dual-glo luciferase reporter gene assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Retinoic acid receptor RXR-alpha (CHEMBL2061)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation.
Pollinger J, Gellrich L, Schierle S, Kilu W, Schmidt J, Kalinowsky L, Ohrndorf J, Kaiser A, Heering J, Proschak E, Merk D.
J Med Chem (2019) 62 : 2112 -2126
PubMed 30702885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 5.23 7.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4558880 1 7.03
CHEMBL4518775 1 6.02
CHEMBL4575123 1 5.85
CHEMBL459521 1 5.82
CHEMBL4458208 1 5.68
CHEMBL44078 1 5.55
CHEMBL42489 1 5.33
CHEMBL4443400 1 5.21
CHEMBL4439891 1 5.17
CHEMBL4533202 1 5.14
CHEMBL295416 PIRINIXIC ACID 2.0 1 5.04
CHEMBL4459701 1 5.02
CHEMBL4465004 1 5.01
CHEMBL4548975 1 5.00
CHEMBL512563 1 4.89
CHEMBL4439052 1 4.70
CHEMBL4514313 1 4.60
CHEMBL454691 1 4.57
CHEMBL4556277 1 4.52
CHEMBL4471255 1 4.44
CHEMBL274797 1 -
CHEMBL461409 1 -
CHEMBL459972 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4558880 EC50 = 93.0 nM 7.03
CHEMBL4518775 EC50 = 950.0 nM 6.02
CHEMBL4575123 EC50 = 1400.0 nM 5.85
CHEMBL459521 EC50 = 1500.0 nM 5.82
CHEMBL4458208 EC50 = 2100.0 nM 5.68
CHEMBL44078 EC50 = 2800.0 nM 5.55
CHEMBL42489 EC50 = 4700.0 nM 5.33
CHEMBL4443400 EC50 = 6100.0 nM 5.21
CHEMBL4439891 EC50 = 6800.0 nM 5.17
CHEMBL4533202 EC50 = 7300.0 nM 5.14
CHEMBL295416 PIRINIXIC ACID EC50 = 9100.0 nM 5.04
CHEMBL4459701 EC50 = 9600.0 nM 5.02
CHEMBL4465004 EC50 = 9800.0 nM 5.01
CHEMBL4548975 EC50 = 10000.0 nM 5.00
CHEMBL512563 EC50 = 13000.0 nM 4.89
CHEMBL4439052 EC50 = 19800.0 nM 4.70
CHEMBL4514313 EC50 = 25000.0 nM 4.60
CHEMBL454691 EC50 = 27000.0 nM 4.57
CHEMBL4556277 EC50 = 30200.0 nM 4.52
CHEMBL4471255 EC50 = 36400.0 nM 4.44
CHEMBL274797 EC50 - -
CHEMBL461409 EC50 - -
CHEMBL459972 EC50 - -