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Assay Detail

CHEMBL4322386

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

Binding
Agonist activity at human full length LRH1 transfected in human HeLa cells incubated for 24 hrs by renilla luciferase reporter gene assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Nuclear receptor subfamily 5 group A member 2 (CHEMBL3544)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of the First Low Nanomolar Liver Receptor Homolog-1 Agonist through Structure-guided Design.
Mays SG, Flynn AR, Cornelison JL, Okafor CD, Wang H, Wang G, Huang X, Donaldson HN, Millings EJ, Polavarapu R, Moore DD, Calvert JW, Jui NT, Ortlund EA.
J Med Chem (2019) 62 : 11022 -11034
PubMed 31419141 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 32 6.03 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4440757 1 7.82
CHEMBL4447391 1 7.40
CHEMBL4565513 1 7.00
CHEMBL4541939 1 6.30
CHEMBL4558553 1 6.10
CHEMBL4455426 1 6.10
CHEMBL4461328 1 6.05
CHEMBL4452061 1 6.05
CHEMBL4460749 1 6.00
CHEMBL1765959 1 5.82
CHEMBL4471992 1 5.70
CHEMBL4562317 1 5.52
CHEMBL4574667 1 5.40
CHEMBL4527695 1 5.30
CHEMBL4514240 1 5.05
CHEMBL4559668 1 4.89
CHEMBL4458433 1 -
CHEMBL4569459 1 -
CHEMBL4465557 1 -
CHEMBL4587527 1 -
CHEMBL4557693 1 -
CHEMBL4532173 1 -
CHEMBL4452639 1 -
CHEMBL4555039 1 -
CHEMBL4558333 1 -
CHEMBL4552141 1 -
CHEMBL4569856 1 -
CHEMBL4572760 1 -
CHEMBL4435095 1 -
CHEMBL4464683 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4440757 EC50 = 15.0 nM 7.82
CHEMBL4447391 EC50 = 40.0 nM 7.40
CHEMBL4565513 EC50 = 100.0 nM 7.00
CHEMBL4541939 EC50 = 500.0 nM 6.30
CHEMBL4558553 EC50 = 800.0 nM 6.10
CHEMBL4455426 EC50 = 800.0 nM 6.10
CHEMBL4461328 EC50 = 900.0 nM 6.05
CHEMBL4452061 EC50 = 900.0 nM 6.05
CHEMBL4460749 EC50 = 1000.0 nM 6.00
CHEMBL1765959 EC50 = 1500.0 nM 5.82
CHEMBL4471992 EC50 = 2000.0 nM 5.70
CHEMBL4562317 EC50 = 3000.0 nM 5.52
CHEMBL4574667 EC50 = 4000.0 nM 5.40
CHEMBL4527695 EC50 = 5000.0 nM 5.30
CHEMBL4514240 EC50 = 9000.0 nM 5.05
CHEMBL4559668 EC50 = 13000.0 nM 4.89
CHEMBL4566367 EC50 - -
CHEMBL4464206 EC50 - -
CHEMBL4464683 EC50 - -
CHEMBL4435095 EC50 - -
CHEMBL4572760 EC50 - -
CHEMBL4569856 EC50 - -
CHEMBL4552141 EC50 - -
CHEMBL4558333 EC50 - -
CHEMBL4555039 EC50 - -
CHEMBL4452639 EC50 - -
CHEMBL4532173 EC50 - -
CHEMBL4557693 EC50 - -
CHEMBL4587527 EC50 - -
CHEMBL4465557 EC50 - -
CHEMBL4569459 EC50 - -
CHEMBL4458433 EC50 - -