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Assay Detail

CHEMBL2071936

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

Binding
Activation of Kv7.1 channel expressed in CHO cells assessed as depolarization-induced thallium influx after 3 mins by patch clamp assay
64
Total Activities
64
Compounds Tested
2
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

Target

Potassium voltage-gated channel subfamily KQT member 1 (CHEMBL1866)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator.
Mattmann ME, Yu H, Lin Z, Xu K, Huang X, Long S, Wu M, McManus OB, Engers DW, Le UM, Li M, Lindsley CW, Hopkins CR.
Bioorg Med Chem Lett (2012) 22 : 5936 -5941
PubMed 22910039 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 63 5.76 6.58
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2070953 1 6.58
CHEMBL2070970 1 6.38
CHEMBL2070988 1 6.22
CHEMBL2070954 1 6.16
CHEMBL2070968 1 6.14
CHEMBL2070962 1 6.11
CHEMBL2070961 1 6.09
CHEMBL2070964 1 6.06
CHEMBL2070952 1 6.05
CHEMBL2070958 1 6.00
CHEMBL2070967 1 5.99
CHEMBL2070966 1 5.94
CHEMBL2071004 1 5.88
CHEMBL2070978 1 5.87
CHEMBL2070832 1 5.86
CHEMBL2070969 1 5.85
CHEMBL2070830 1 5.83
CHEMBL2070965 1 5.79
CHEMBL2070959 1 5.77
CHEMBL1352968 1 5.77
CHEMBL2070960 1 5.75
CHEMBL2070955 1 5.59
CHEMBL2070985 1 5.54
CHEMBL2070987 1 5.36
CHEMBL2070957 1 5.32
CHEMBL2070981 1 5.21
CHEMBL2070977 1 5.10
CHEMBL2070982 1 5.09
CHEMBL2070995 1 4.89
CHEMBL2071006 1 4.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2070953 EC50 = 260.0 nM 6.58
CHEMBL2070970 EC50 = 420.0 nM 6.38
CHEMBL2070988 EC50 = 600.0 nM 6.22
CHEMBL2070954 EC50 = 700.0 nM 6.16
CHEMBL2070968 EC50 = 730.0 nM 6.14
CHEMBL2070962 EC50 = 780.0 nM 6.11
CHEMBL2070961 EC50 = 810.0 nM 6.09
CHEMBL2070964 EC50 = 880.0 nM 6.06
CHEMBL2070952 EC50 = 890.0 nM 6.05
CHEMBL2070958 EC50 = 1000.0 nM 6.00
CHEMBL2070967 EC50 = 1030.0 nM 5.99
CHEMBL2070966 EC50 = 1160.0 nM 5.94
CHEMBL2071004 EC50 = 1320.0 nM 5.88
CHEMBL2070978 EC50 = 1360.0 nM 5.87
CHEMBL2070832 EC50 = 1380.0 nM 5.86
CHEMBL2070969 EC50 = 1410.0 nM 5.85
CHEMBL2070830 EC50 = 1470.0 nM 5.83
CHEMBL2070965 EC50 = 1630.0 nM 5.79
CHEMBL2070959 EC50 = 1710.0 nM 5.77
CHEMBL1352968 EC50 = 1690.0 nM 5.77
CHEMBL2070960 EC50 = 1780.0 nM 5.75
CHEMBL2070955 EC50 = 2590.0 nM 5.59
CHEMBL2070985 EC50 = 2860.0 nM 5.54
CHEMBL2070987 EC50 = 4380.0 nM 5.36
CHEMBL2070957 EC50 = 4740.0 nM 5.32
CHEMBL2070981 EC50 = 6130.0 nM 5.21
CHEMBL2070977 EC50 = 7970.0 nM 5.10
CHEMBL2070982 EC50 = 8160.0 nM 5.09
CHEMBL2070995 EC50 = 12900.0 nM 4.89
CHEMBL2071006 EC50 = 27400.0 nM 4.56
CHEMBL2070971 EC50 > 30000.0 nM -
CHEMBL2070963 EC50 > 30000.0 nM -
CHEMBL2070956 EC50 > 30000.0 nM -
CHEMBL2070831 EC50 > 30000.0 nM -
CHEMBL2070979 EC50 > 30000.0 nM -
CHEMBL2071009 EC50 > 30000.0 nM -
CHEMBL2071010 EC50 > 30000.0 nM -
CHEMBL2071008 EC50 > 30000.0 nM -
CHEMBL2071007 EC50 > 30000.0 nM -
CHEMBL2071005 EC50 > 30000.0 nM -
CHEMBL2071003 EC50 > 30000.0 nM -
CHEMBL2071001 EC50 > 30000.0 nM -
CHEMBL2071000 EC50 > 30000.0 nM -
CHEMBL2070999 EC50 > 30000.0 nM -
CHEMBL2070994 EC50 > 30000.0 nM -
CHEMBL2070996 EC50 > 30000.0 nM -
CHEMBL2070997 EC50 > 30000.0 nM -
CHEMBL2071002 EC50 > 30000.0 nM -
CHEMBL2070998 EC50 > 30000.0 nM -
CHEMBL2071011 Activity - -