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Assay Detail

CHEMBL4835415

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Binding
Agonist activity at human RXRalpha transfected in human HEK293T cells co-expressing pFR/pRL-Luc incubated for 14 to 16 hrs by hybrid reporter gene assay
ChEMBL ↗
43
Total Activities
43
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Oxaprozin Analogues as Selective RXR Agonists with Superior Properties and Pharmacokinetics.
Schierle S, Chaikuad A, Lillich FF, Ni X, Woltersdorf S, Schallmayer E, Renelt B, Ronchetti R, Knapp S, Proschak E, Merk D.
J Med Chem (2021) 64 : 5123 -5136
PubMed 33793232 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 42 5.91 7.30
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4855847 — — 1 7.30
CHEMBL4874191 — — 1 7.22
CHEMBL4876667 — — 1 7.16
CHEMBL4446467 — — 1 6.89
CHEMBL4879068 — — 1 6.75
CHEMBL4862605 — — 1 6.60
CHEMBL4855868 — — 1 6.52
CHEMBL4854458 — — 1 6.52
CHEMBL4849999 — — 1 6.52
CHEMBL4849776 — — 1 6.37
CHEMBL4855407 — — 1 6.36
CHEMBL4868343 — — 1 6.32
CHEMBL4875485 — — 1 6.30
CHEMBL4859732 — — 1 6.30
CHEMBL4852349 — — 1 6.29
CHEMBL4471300 — — 1 6.21
CHEMBL4865656 — — 1 6.17
CHEMBL4873606 — — 1 6.16
CHEMBL4846058 — — 1 6.00
CHEMBL4872307 — — 1 5.99
CHEMBL4873831 — — 1 5.92
CHEMBL4867027 — — 1 5.89
CHEMBL4515740 — — 1 5.89
CHEMBL4864263 — — 1 5.85
CHEMBL4862395 — — 1 5.80
CHEMBL4878182 — — 1 5.72
CHEMBL4848283 — — 1 5.60
CHEMBL4866557 — — 1 5.51
CHEMBL4851869 — — 1 5.44
CHEMBL4873561 — — 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4855847 — EC50 = 50.0 nM 7.30
CHEMBL4874191 — EC50 = 60.0 nM 7.22
CHEMBL4876667 — EC50 = 70.0 nM 7.16
CHEMBL4446467 — EC50 = 130.0 nM 6.89
CHEMBL4879068 — EC50 = 180.0 nM 6.75
CHEMBL4862605 — EC50 = 250.0 nM 6.60
CHEMBL4855868 — EC50 = 300.0 nM 6.52
CHEMBL4854458 — EC50 = 300.0 nM 6.52
CHEMBL4849999 — EC50 = 300.0 nM 6.52
CHEMBL4849776 — EC50 = 430.0 nM 6.37
CHEMBL4855407 — EC50 = 440.0 nM 6.36
CHEMBL4868343 — EC50 = 480.0 nM 6.32
CHEMBL4875485 — EC50 = 500.0 nM 6.30
CHEMBL4859732 — EC50 = 500.0 nM 6.30
CHEMBL4852349 — EC50 = 510.0 nM 6.29
CHEMBL4471300 — EC50 = 620.0 nM 6.21
CHEMBL4865656 — EC50 = 680.0 nM 6.17
CHEMBL4873606 — EC50 = 700.0 nM 6.16
CHEMBL4846058 — EC50 = 1000.0 nM 6.00
CHEMBL4872307 — EC50 = 1030.0 nM 5.99
CHEMBL4873831 — EC50 = 1200.0 nM 5.92
CHEMBL4867027 — EC50 = 1300.0 nM 5.89
CHEMBL4515740 — EC50 = 1300.0 nM 5.89
CHEMBL4864263 — EC50 = 1400.0 nM 5.85
CHEMBL4862395 — EC50 = 1600.0 nM 5.80
CHEMBL4878182 — EC50 = 1900.0 nM 5.72
CHEMBL4848283 — EC50 = 2500.0 nM 5.60
CHEMBL4866557 — EC50 = 3100.0 nM 5.51
CHEMBL4851869 — EC50 = 3600.0 nM 5.44
CHEMBL4873561 — EC50 = 4000.0 nM 5.40
CHEMBL4860614 — EC50 = 5800.0 nM 5.24
CHEMBL4847503 — EC50 = 6500.0 nM 5.19
CHEMBL4867317 — EC50 = 7700.0 nM 5.11
CHEMBL333698 — EC50 = 7900.0 nM 5.10
CHEMBL331916 — EC50 = 8400.0 nM 5.08
CHEMBL4861965 — EC50 = 9900.0 nM 5.00
CHEMBL1071 OXAPROZIN EC50 = 16100.0 nM 4.79
CHEMBL4863720 — EC50 = 16900.0 nM 4.77
CHEMBL4858779 — EC50 = 17000.0 nM 4.77
CHEMBL4439422 — EC50 = 36000.0 nM 4.44
CHEMBL4874180 — EC50 > 30000.0 nM -
CHEMBL4855573 — Activity - — -
CHEMBL4847339 — EC50 > 50000.0 nM -