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Assay Detail

CHEMBL901965

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

Binding
Channel opening activity at human bladder Kir6.2 channel containing SUR2B expressed in L cells by FLIPR assay
ChEMBL ↗
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

ATP-sensitive inward rectifier potassium channel 11 (CHEMBL1886) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity studies of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.
Perez-Medrano A, Brune ME, Buckner SA, Coghlan MJ, Fey TA, Gopalakrishnan M, Gregg RJ, Kort ME, Scott VE, Sullivan JP, Whiteaker KL, Carroll WA.
J Med Chem (2007) 50 : 6265 -6273
PubMed 17973362 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 57 5.62 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL239512 — — 1 6.47
CHEMBL18861 ZD-6169 — 1 6.36
CHEMBL239514 — — 1 6.34
CHEMBL391369 — — 1 6.27
CHEMBL393831 — — 1 6.19
CHEMBL238883 — — 1 6.12
CHEMBL241199 — — 1 6.11
CHEMBL239119 — — 1 6.09
CHEMBL239121 — — 1 6.05
CHEMBL239128 — — 1 6.04
CHEMBL393424 — — 1 6.02
CHEMBL274449 — — 1 5.97
CHEMBL241200 — — 1 5.96
CHEMBL410755 — — 1 5.96
CHEMBL393730 — — 1 5.93
CHEMBL397830 — — 1 5.89
CHEMBL241409 — — 1 5.89
CHEMBL393425 — — 1 5.88
CHEMBL238884 — — 1 5.82
CHEMBL239090 — — 1 5.79
CHEMBL241410 — — 1 5.78
CHEMBL240135 — — 1 5.78
CHEMBL395452 — — 1 5.77
CHEMBL240560 — — 1 5.76
CHEMBL238422 — — 1 5.69
CHEMBL240131 — — 1 5.69
CHEMBL240766 — — 1 5.68
CHEMBL2110262 — — 1 5.67
CHEMBL395175 — — 1 5.65
CHEMBL393731 — — 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL239512 — EC50 = 338.84 nM 6.47
CHEMBL18861 ZD-6169 EC50 = 436.52 nM 6.36
CHEMBL239514 — EC50 = 457.09 nM 6.34
CHEMBL391369 — EC50 = 537.03 nM 6.27
CHEMBL393831 — EC50 = 645.65 nM 6.19
CHEMBL238883 — EC50 = 758.58 nM 6.12
CHEMBL241199 — EC50 = 776.25 nM 6.11
CHEMBL239119 — EC50 = 812.83 nM 6.09
CHEMBL239121 — EC50 = 891.25 nM 6.05
CHEMBL239128 — EC50 = 912.01 nM 6.04
CHEMBL393424 — EC50 = 954.99 nM 6.02
CHEMBL274449 — EC50 = 1071.52 nM 5.97
CHEMBL410755 — EC50 = 1096.48 nM 5.96
CHEMBL241200 — EC50 = 1096.48 nM 5.96
CHEMBL393730 — EC50 = 1174.9 nM 5.93
CHEMBL397830 — EC50 = 1288.25 nM 5.89
CHEMBL241409 — EC50 = 1288.25 nM 5.89
CHEMBL393425 — EC50 = 1318.26 nM 5.88
CHEMBL238884 — EC50 = 1513.56 nM 5.82
CHEMBL239090 — EC50 = 1621.81 nM 5.79
CHEMBL241410 — EC50 = 1659.59 nM 5.78
CHEMBL240135 — EC50 = 1659.59 nM 5.78
CHEMBL395452 — EC50 = 1698.24 nM 5.77
CHEMBL240560 — EC50 = 1737.8 nM 5.76
CHEMBL240131 — EC50 = 2041.74 nM 5.69
CHEMBL238422 — EC50 = 2041.74 nM 5.69
CHEMBL240766 — EC50 = 2089.3 nM 5.68
CHEMBL2110262 — EC50 = 2137.96 nM 5.67
CHEMBL395175 — EC50 = 2238.72 nM 5.65
CHEMBL393731 — EC50 = 2290.87 nM 5.64
CHEMBL238638 — EC50 = 2290.87 nM 5.64
CHEMBL240767 — EC50 = 2570.4 nM 5.59
CHEMBL241411 — EC50 = 2630.27 nM 5.58
CHEMBL240345 — EC50 = 2754.23 nM 5.56
CHEMBL240768 — EC50 = 3715.35 nM 5.43
CHEMBL240988 — EC50 = 3801.89 nM 5.42
CHEMBL238640 — EC50 = 4265.8 nM 5.37
CHEMBL238854 — EC50 = 4265.8 nM 5.37
CHEMBL238639 — EC50 = 4265.8 nM 5.37
CHEMBL436805 — EC50 = 4570.88 nM 5.34
CHEMBL240346 — EC50 = 5011.87 nM 5.30
CHEMBL395453 — EC50 = 5370.32 nM 5.27
CHEMBL240347 — EC50 = 5370.32 nM 5.27
CHEMBL540965 — EC50 = 6025.6 nM 5.22
CHEMBL240558 — EC50 = 6606.93 nM 5.18
CHEMBL392290 — EC50 = 6760.83 nM 5.17
CHEMBL240989 — EC50 = 7762.47 nM 5.11
CHEMBL240559 — EC50 = 8912.51 nM 5.05
CHEMBL393952 — EC50 = 8912.51 nM 5.05
CHEMBL393130 — EC50 = 9549.93 nM 5.02