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Assay Detail

CHEMBL701214

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Functional
Evaluated for K-ATP activity in terms of membrane potential change, through guinea pig bladder assay
ChEMBL ↗
54
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Sulfonylurea receptors; K-ATP channels (CHEMBL2095152) ↗
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of a novel series of tricyclic dihydropyridine-based KATP openers that potently inhibit bladder contractions in vitro.
Carroll WA, Agrios KA, Altenbach RJ, Buckner SA, Chen Y, Coghlan MJ, Daza AV, Drizin I, Gopalakrishnan M, Henry RF, Kort ME, Kym PR, Milicic I, Smith JC, Tang R, Turner SC, Whiteaker KL, Zhang H, Sullivan JP.
J Med Chem (2004) 47 : 3180 -3192
PubMed 15163197 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 54 6.78 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL321455 — — 1 9.27
CHEMBL3138573 — — 1 8.30
CHEMBL323159 — — 1 8.20
CHEMBL3392139 — — 2 8.06
CHEMBL2111694 — — 1 7.95
CHEMBL108723 — — 1 7.89
CHEMBL108251 — — 1 7.85
CHEMBL107888 — — 1 7.65
CHEMBL2112487 — — 1 7.59
CHEMBL320983 — — 1 7.57
CHEMBL321210 — — 1 7.50
CHEMBL108440 — — 1 7.45
CHEMBL3138579 — — 1 7.27
CHEMBL109412 — — 1 7.20
CHEMBL110399 — — 1 7.20
CHEMBL110511 — — 1 7.19
CHEMBL323787 — — 1 7.17
CHEMBL3392140 — — 1 7.14
CHEMBL326901 — — 1 7.10
CHEMBL108969 — — 1 7.09
CHEMBL320931 — — 1 6.97
CHEMBL108547 — — 1 6.94
CHEMBL111297 — — 1 6.93
CHEMBL323397 — — 1 6.85
CHEMBL106755 — — 1 6.75
CHEMBL109693 — — 2 6.73
CHEMBL108029 — — 1 6.68
CHEMBL107933 — — 1 6.63
CHEMBL106984 — — 1 6.55
CHEMBL326016 — — 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL321455 — EC50 = 0.537 nM 9.27
CHEMBL3138573 — EC50 = 5.012 nM 8.30
CHEMBL323159 — EC50 = 6.31 nM 8.20
CHEMBL3392139 — EC50 = 8.71 nM 8.06
CHEMBL2111694 — EC50 = 11.22 nM 7.95
CHEMBL108723 — EC50 = 12.88 nM 7.89
CHEMBL108251 — EC50 = 14.13 nM 7.85
CHEMBL107888 — EC50 = 22.39 nM 7.65
CHEMBL2112487 — EC50 = 25.7 nM 7.59
CHEMBL320983 — EC50 = 26.92 nM 7.57
CHEMBL321210 — EC50 = 31.62 nM 7.50
CHEMBL108440 — EC50 = 35.48 nM 7.45
CHEMBL3138579 — EC50 = 53.7 nM 7.27
CHEMBL109412 — EC50 = 63.1 nM 7.20
CHEMBL110399 — EC50 = 63.1 nM 7.20
CHEMBL110511 — EC50 = 64.57 nM 7.19
CHEMBL323787 — EC50 = 67.61 nM 7.17
CHEMBL3392140 — EC50 = 72.44 nM 7.14
CHEMBL326901 — EC50 = 79.43 nM 7.10
CHEMBL108969 — EC50 = 81.28 nM 7.09
CHEMBL320931 — EC50 = 107.15 nM 6.97
CHEMBL108547 — EC50 = 114.82 nM 6.94
CHEMBL111297 — EC50 = 117.49 nM 6.93
CHEMBL323397 — EC50 = 141.25 nM 6.85
CHEMBL106755 — EC50 = 177.83 nM 6.75
CHEMBL109693 — EC50 = 186.21 nM 6.73
CHEMBL108029 — EC50 = 208.93 nM 6.68
CHEMBL107933 — EC50 = 234.42 nM 6.63
CHEMBL106984 — EC50 = 281.84 nM 6.55
CHEMBL326016 — EC50 = 316.23 nM 6.50
CHEMBL320518 — EC50 = 398.11 nM 6.40
CHEMBL3138558 — EC50 = 416.87 nM 6.38
CHEMBL11684 (-)-CROMAKALIM EC50 = 426.58 nM 6.37
CHEMBL322931 — EC50 = 436.52 nM 6.36
CHEMBL320337 — EC50 = 537.03 nM 6.27
CHEMBL111204 — EC50 = 537.03 nM 6.27
CHEMBL106033 — EC50 = 562.34 nM 6.25
CHEMBL325571 — EC50 = 575.44 nM 6.24
CHEMBL324618 — EC50 = 691.83 nM 6.16
CHEMBL108816 — EC50 = 691.83 nM 6.16
CHEMBL108400 — EC50 = 977.24 nM 6.01
CHEMBL110987 — EC50 = 1000.0 nM 6.00
CHEMBL109693 — EC50 = 1023.29 nM 5.99
CHEMBL323460 — EC50 = 1096.48 nM 5.96
CHEMBL322507 — EC50 = 1230.27 nM 5.91
CHEMBL3138562 — EC50 = 1380.38 nM 5.86
CHEMBL3138551 — EC50 = 2570.4 nM 5.59
CHEMBL108658 — EC50 = 2630.27 nM 5.58
CHEMBL432204 — EC50 = 2818.38 nM 5.55
CHEMBL325571 — EC50 = 5011.87 nM 5.30