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Assay Detail

CHEMBL4386458

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Binding
Inhibition of human ERG expressed in CHOK1 cells assessed as reduction in tail current amplitude by automated patch-clamp method
2
Total Activities
2
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

Publication

Difluoromethylene at the γ-Lactam α-Position Improves 11-Deoxy-8-aza-PGE<sub>1</sub> Series EP<sub>4</sub> Receptor Binding and Activity: 11-Deoxy-10,10-difluoro-8-aza-PGE<sub>1</sub> Analog (KMN-159) as a Potent EP<sub>4</sub> Agonist.
Barrett SD, Holt MC, Kramer JB, Germain B, Ho CS, Ciske FL, Kornilov A, Colombo JM, Uzieblo A, O'Malley JP, Owen TA, Stein AJ, Morano MI.
J Med Chem (2019) 62 : 4731 -4741
PubMed 30964292 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.57 4.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3918816 1 4.59
CHEMBL4558749 1 4.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3918816 IC50 = 25900.0 nM 4.59
CHEMBL4558749 IC50 = 29000.0 nM 4.54