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Assay Detail

CHEMBL4384747

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Binding
Inhibition of human ERG expressed in CHO cells by Qpatch assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid-4 with in Vivo Activity in a Pulmonary Edema Model.
Pero JE, Matthews JM, Behm DJ, Brnardic EJ, Brooks C, Budzik BW, Costell MH, Donatelli CA, Eisennagel SH, Erhard K, Fischer MC, Holt DA, Jolivette LJ, Li H, Li P, McAtee JJ, McCleland BW, Pendrak I, Posobiec LM, Rivera KLK, Rivero RA, Roethke TJ, Sender MR, Shu A, Terrell LR, Vaidya K, Xu X, Lawhorn BG.
J Med Chem (2018) 61 : 11209 -11220
PubMed 30500190 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.16 5.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4456312 1 5.28
CHEMBL4547537 1 5.10
CHEMBL4461475 1 5.10
CHEMBL4439190 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4456312 IC50 = 5300.0 nM 5.28
CHEMBL4547537 IC50 = 8000.0 nM 5.10
CHEMBL4461475 IC50 = 8000.0 nM 5.10
CHEMBL4439190 IC50 > 10000.0 nM -