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Assay Detail

CHEMBL906905

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

Functional
Agonist activity at NR2E3 by luciferase NCOR release assay in CHO cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Photoreceptor-specific nuclear receptor (CHEMBL4374)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand.
Wolkenberg SE, Zhao Z, Kapitskaya M, Webber AL, Petrukhin K, Tang YS, Dean DC, Hartman GD, Lindsley CW.
Bioorg Med Chem Lett (2006) 16 : 5001 -5004
PubMed 16879962 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 5.96 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386138 1 7.46
CHEMBL213426 1 6.83
CHEMBL384623 1 6.77
CHEMBL212336 1 6.58
CHEMBL213665 1 6.48
CHEMBL214562 1 6.43
CHEMBL215539 1 6.21
CHEMBL214445 1 6.01
CHEMBL424715 1 5.88
CHEMBL384232 1 5.66
CHEMBL214374 1 5.58
CHEMBL385936 1 5.54
CHEMBL214457 1 5.52
CHEMBL386087 1 5.39
CHEMBL384066 1 5.39
CHEMBL386447 1 5.38
CHEMBL215363 1 5.14
CHEMBL215498 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386138 EC50 = 35.0 nM 7.46
CHEMBL213426 EC50 = 147.0 nM 6.83
CHEMBL384623 EC50 = 170.0 nM 6.77
CHEMBL212336 EC50 = 260.0 nM 6.58
CHEMBL213665 EC50 = 330.0 nM 6.48
CHEMBL214562 EC50 = 370.0 nM 6.43
CHEMBL215539 EC50 = 610.0 nM 6.21
CHEMBL214445 EC50 = 986.0 nM 6.01
CHEMBL424715 EC50 = 1320.0 nM 5.88
CHEMBL384232 EC50 = 2200.0 nM 5.66
CHEMBL214374 EC50 = 2610.0 nM 5.58
CHEMBL385936 EC50 = 2900.0 nM 5.54
CHEMBL214457 EC50 = 3000.0 nM 5.52
CHEMBL386087 EC50 = 4100.0 nM 5.39
CHEMBL384066 EC50 = 4100.0 nM 5.39
CHEMBL386447 EC50 = 4200.0 nM 5.38
CHEMBL215363 EC50 = 7200.0 nM 5.14
CHEMBL215498 EC50 = 10000.0 nM 5.00