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Assay Detail

CHEMBL1767448

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

Functional
Agonist activity at human LRH-1 receptor assessed as TIF2 737-757 peptide recruitment by TR-FRET assay relative to control
ChEMBL ↗
46
Total Activities
46
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
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

Small molecule agonists of the orphan nuclear receptors steroidogenic factor-1 (SF-1, NR5A1) and liver receptor homologue-1 (LRH-1, NR5A2).
Whitby RJ, Stec J, Blind RD, Dixon S, Leesnitzer LM, Orband-Miller LA, Williams SP, Willson TM, Xu R, Zuercher WJ, Cai F, Ingraham HA.
J Med Chem (2011) 54 : 2266 -2281
PubMed 21391689 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 31 6.17 7.50
pEC50 15 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL384153 — — 1 7.50
CHEMBL1765932 — — 1 7.00
CHEMBL1765955 — — 1 6.80
CHEMBL1765953 — — 1 6.70
CHEMBL1765956 — — 1 6.60
CHEMBL1765933 — — 1 6.60
CHEMBL1765945 — — 1 6.60
CHEMBL1765959 — — 1 6.60
CHEMBL1765962 — — 1 6.60
CHEMBL1765934 — — 1 6.50
CHEMBL1765958 — — 1 6.50
CHEMBL1765960 — — 1 6.40
CHEMBL1765961 — — 1 6.40
CHEMBL1765966 — — 1 6.30
CHEMBL385911 — — 1 6.20
CHEMBL1765951 — — 1 6.10
CHEMBL1765931 — — 1 6.10
CHEMBL1765963 — — 1 6.00
CHEMBL1765938 — — 1 6.00
CHEMBL1765957 — — 1 5.90
CHEMBL1765950 — — 1 5.90
CHEMBL1765964 — — 1 5.80
CHEMBL1765954 — — 1 5.80
CHEMBL1765936 — — 1 5.70
CHEMBL1765942 — — 1 5.60
CHEMBL1765930 — — 1 5.60
CHEMBL1765927 — — 1 5.60
CHEMBL1765926 — — 1 5.60
CHEMBL1765941 — — 1 5.50
CHEMBL1765928 — — 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL384153 — EC50 = 31.62 nM 7.50
CHEMBL1765932 — EC50 = 100.0 nM 7.00
CHEMBL1765955 — EC50 = 158.49 nM 6.80
CHEMBL1765953 — EC50 = 199.53 nM 6.70
CHEMBL1765956 — EC50 = 251.19 nM 6.60
CHEMBL1765933 — EC50 = 251.19 nM 6.60
CHEMBL1765945 — EC50 = 251.19 nM 6.60
CHEMBL1765959 — EC50 = 251.19 nM 6.60
CHEMBL1765962 — EC50 = 251.19 nM 6.60
CHEMBL1765934 — EC50 = 316.23 nM 6.50
CHEMBL1765958 — EC50 = 316.23 nM 6.50
CHEMBL1765960 — EC50 = 398.11 nM 6.40
CHEMBL1765961 — EC50 = 398.11 nM 6.40
CHEMBL1765966 — EC50 = 501.19 nM 6.30
CHEMBL385911 — EC50 = 630.96 nM 6.20
CHEMBL1765951 — EC50 = 794.33 nM 6.10
CHEMBL1765931 — EC50 = 794.33 nM 6.10
CHEMBL1765963 — EC50 = 1000.0 nM 6.00
CHEMBL1765938 — EC50 = 1000.0 nM 6.00
CHEMBL1765957 — EC50 = 1258.93 nM 5.90
CHEMBL1765950 — EC50 = 1258.93 nM 5.90
CHEMBL1765964 — EC50 = 1584.89 nM 5.80
CHEMBL1765954 — EC50 = 1584.89 nM 5.80
CHEMBL1765936 — EC50 = 1995.26 nM 5.70
CHEMBL1765930 — EC50 = 2511.89 nM 5.60
CHEMBL1765927 — EC50 = 2511.89 nM 5.60
CHEMBL1765926 — EC50 = 2511.89 nM 5.60
CHEMBL1765942 — EC50 = 2511.89 nM 5.60
CHEMBL1765941 — EC50 = 3162.28 nM 5.50
CHEMBL1765928 — EC50 = 3162.28 nM 5.50
CHEMBL1765929 — EC50 = 5011.87 nM 5.30
CHEMBL1765965 — pEC50 - — -
CHEMBL1765952 — pEC50 - — -
CHEMBL1765949 — pEC50 - — -
CHEMBL1765948 — pEC50 - — -
CHEMBL1765947 — pEC50 - — -
CHEMBL1765946 — pEC50 - — -
CHEMBL1765944 — pEC50 - — -
CHEMBL1765943 — pEC50 - — -
CHEMBL1765940 — pEC50 - — -
CHEMBL1765939 — pEC50 - — -
CHEMBL1765937 — pEC50 - — -
CHEMBL1765935 — pEC50 - — -
CHEMBL1765924 — pEC50 - — -
CHEMBL1765923 — pEC50 - — -
CHEMBL1765925 — pEC50 - — -