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Assay Detail

CHEMBL5516904

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

Toxicity
Inhibition of human ERG expressed in HEK293 cells incubated for 2 to 5 mins by Manual patch clamp assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Toxicity
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery of BMS-986308: A Renal Outer Medullary Potassium Channel Inhibitor for the Treatment of Heart Failure.
Richter JM, Gunaga P, Yadav N, Bora RO, Bhide R, Rajugowda N, Govindrajulu K, Godesi S, Akuthota N, Rao P, Sivaraman A, Panda M, Kaspady M, Gupta A, Mathur A, Levesque PC, Gulia J, Dokania M, Ramarao M, Kole P, Chacko S, Lentz KA, Sivaprasad Lvj S, Thatipamula RP, Sridhar S, Kamble S, Govindrajan A, Soleman SI, Gordon DA, Wexler RR, Priestley ES.
J Med Chem (2024) 67 : 9731 -9744
PubMed 38807539 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.85 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5560486 1 8.00
CHEMBL5560628 1 6.39
CHEMBL5561980 1 5.44
CHEMBL5563848 1 4.75
CHEMBL5561669 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5560486 IC50 = 10.0 nM 8.00
CHEMBL5560628 IC50 = 410.0 nM 6.39
CHEMBL5561980 IC50 = 3600.0 nM 5.44
CHEMBL5563848 IC50 = 18000.0 nM 4.75
CHEMBL5561669 IC50 = 21000.0 nM 4.68