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Assay Detail

CHEMBL686880

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

Functional
Inhibition of Iks current in isolated guinea pig myocytes during a 1s voltage clamp step from -50 to +50 mV.
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]acetamide.
Selnick HG, Liverton NJ, Baldwin JJ, Butcher JW, Claremon DA, Elliott JM, Freidinger RM, King SA, Libby BE, McIntyre CJ, Pribush DA, Remy DC, Smith GR, Tebben AJ, Jurkiewicz NK, Lynch JJ, Salata JJ, Sanguinetti MC, Siegl PK, Slaughter DE, Vyas K.
J Med Chem (1997) 40 : 3865 -3868
PubMed 9397166 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.08 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL332826 1 8.22
CHEMBL126716 1 8.22
CHEMBL16900 L-768673 1 8.22
CHEMBL127701 1 8.05
CHEMBL441474 1 8.00
CHEMBL340353 1 8.00
CHEMBL127661 1 7.96
CHEMBL443550 1 7.85
CHEMBL126421 1 7.70
CHEMBL339327 1 7.52
CHEMBL331861 1 7.46
CHEMBL127423 1 7.35
CHEMBL341044 1 7.22
CHEMBL330992 1 6.96
CHEMBL124092 1 6.85
CHEMBL124993 1 6.70
CHEMBL9387 L-365260 1 6.67
CHEMBL124306 1 6.52
CHEMBL128007 1 6.28
CHEMBL128031 1 6.22
CHEMBL330970 1 6.00
CHEMBL338109 1 5.55
CHEMBL420516 1 5.36
CHEMBL70380 1 5.00
CHEMBL338217 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL332826 IC50 = 6.0 nM 8.22
CHEMBL126716 IC50 = 6.0 nM 8.22
CHEMBL16900 L-768673 IC50 = 6.0 nM 8.22
CHEMBL127701 IC50 = 9.0 nM 8.05
CHEMBL441474 IC50 = 10.0 nM 8.00
CHEMBL340353 IC50 = 10.0 nM 8.00
CHEMBL127661 IC50 = 11.0 nM 7.96
CHEMBL443550 IC50 = 14.0 nM 7.85
CHEMBL126421 IC50 = 20.0 nM 7.70
CHEMBL339327 IC50 = 30.0 nM 7.52
CHEMBL331861 IC50 = 35.0 nM 7.46
CHEMBL127423 IC50 = 45.0 nM 7.35
CHEMBL341044 IC50 = 60.0 nM 7.22
CHEMBL330992 IC50 = 110.0 nM 6.96
CHEMBL124092 IC50 = 140.0 nM 6.85
CHEMBL124993 IC50 = 200.0 nM 6.70
CHEMBL9387 L-365260 IC50 = 214.0 nM 6.67
CHEMBL124306 IC50 = 300.0 nM 6.52
CHEMBL128007 IC50 = 520.0 nM 6.28
CHEMBL128031 IC50 = 600.0 nM 6.22
CHEMBL330970 IC50 = 1000.0 nM 6.00
CHEMBL338109 IC50 = 2800.0 nM 5.55
CHEMBL420516 IC50 = 4400.0 nM 5.36
CHEMBL70380 IC50 = 10000.0 nM 5.00
CHEMBL338217 IC50 > 10000.0 nM -