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Assay Detail

CHEMBL5516901

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

Binding
Inhibition of human ROMK expressed in T-REX-CHO cells incubated for 30 mins by thallium flux assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

ATP-sensitive inward rectifier potassium channel 1 (CHEMBL1293292)
Type SINGLE PROTEIN
Organism Homo sapiens

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 30 7.53 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5557617 1 9.00
CHEMBL5560084 1 8.18
CHEMBL5560628 1 8.06
CHEMBL5558589 1 7.89
CHEMBL5561980 1 7.89
CHEMBL5559136 1 7.85
CHEMBL5560081 1 7.82
CHEMBL5562228 1 7.82
CHEMBL5560640 1 7.82
CHEMBL5557656 1 7.80
CHEMBL5523625 1 7.77
CHEMBL5565705 1 7.77
CHEMBL5560085 1 7.64
CHEMBL5563848 1 7.62
CHEMBL5560684 1 7.60
CHEMBL5561669 1 7.58
CHEMBL5560876 1 7.52
CHEMBL5556159 1 7.50
CHEMBL5563632 1 7.44
CHEMBL5560041 1 7.34
CHEMBL5556822 1 7.28
CHEMBL5555211 1 7.24
CHEMBL5560486 1 7.23
CHEMBL5558564 1 7.21
CHEMBL5517758 1 7.21
CHEMBL5549890 1 7.13
CHEMBL5555792 1 7.08
CHEMBL5527997 1 7.07
CHEMBL5523626 1 6.37
CHEMBL5556245 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5557617 IC50 = 1.0 nM 9.00
CHEMBL5560084 IC50 = 6.6 nM 8.18
CHEMBL5560628 IC50 = 8.8 nM 8.06
CHEMBL5558589 IC50 = 13.0 nM 7.89
CHEMBL5561980 IC50 = 13.0 nM 7.89
CHEMBL5559136 IC50 = 14.0 nM 7.85
CHEMBL5560081 IC50 = 15.0 nM 7.82
CHEMBL5562228 IC50 = 15.0 nM 7.82
CHEMBL5560640 IC50 = 15.0 nM 7.82
CHEMBL5557656 IC50 = 16.0 nM 7.80
CHEMBL5523625 IC50 = 17.0 nM 7.77
CHEMBL5565705 IC50 = 17.0 nM 7.77
CHEMBL5560085 IC50 = 23.0 nM 7.64
CHEMBL5563848 IC50 = 24.0 nM 7.62
CHEMBL5560684 IC50 = 25.0 nM 7.60
CHEMBL5561669 IC50 = 26.0 nM 7.58
CHEMBL5560876 IC50 = 30.0 nM 7.52
CHEMBL5556159 IC50 = 32.0 nM 7.50
CHEMBL5563632 IC50 = 36.0 nM 7.44
CHEMBL5560041 IC50 = 46.0 nM 7.34
CHEMBL5556822 IC50 = 52.0 nM 7.28
CHEMBL5555211 IC50 = 57.0 nM 7.24
CHEMBL5560486 IC50 = 59.0 nM 7.23
CHEMBL5558564 IC50 = 61.0 nM 7.21
CHEMBL5517758 IC50 = 62.0 nM 7.21
CHEMBL5549890 IC50 = 74.0 nM 7.13
CHEMBL5555792 IC50 = 84.0 nM 7.08
CHEMBL5527997 IC50 = 86.0 nM 7.07
CHEMBL5523626 IC50 = 430.0 nM 6.37
CHEMBL5556245 IC50 = 620.0 nM 6.21