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Assay Detail

CHEMBL701213

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Functional
Evaluated for K-ATP activity in terms of change in membrane potential through guinea pig bladder assay
ChEMBL ↗
69
Total Activities
68
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 2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide K(ATP) channel openers: discovery of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9- hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637), a potent K(ATP) opener that selectively inhibits spontaneous bladder contractions.
Carroll WA, Altenbach RJ, Bai H, Brioni JD, Brune ME, Buckner SA, Cassidy C, Chen Y, Coghlan MJ, Daza AV, Drizin I, Fey TA, Fitzgerald M, Gopalakrishnan M, Gregg RJ, Henry RF, Holladay MW, King LL, Kort ME, Kym PR, Milicic I, Tang R, Turner SC, Whiteaker KL, Yi L, Zhang H, Sullivan JP.
J Med Chem (2004) 47 : 3163 -3179
PubMed 15163196 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 69 6.30 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3138587 — — 1 7.66
CHEMBL3138549 — — 1 7.59
CHEMBL108586 — — 1 7.56
CHEMBL3138545 — — 1 7.55
CHEMBL3138586 — — 1 7.48
CHEMBL3138561 — — 2 7.42
CHEMBL3138553 — — 1 7.36
CHEMBL11458 — — 1 7.35
CHEMBL3138560 — — 1 7.28
CHEMBL3138606 — — 1 7.27
CHEMBL3138596 — — 1 7.26
CHEMBL3138577 — — 1 7.08
CHEMBL3138611 — — 1 6.97
CHEMBL3138607 — — 1 6.91
CHEMBL3138581 — — 1 6.86
CHEMBL3138592 — — 1 6.81
CHEMBL3138548 — — 1 6.74
CHEMBL3138588 — — 1 6.68
CHEMBL3138555 — — 1 6.67
CHEMBL324190 — — 1 6.67
CHEMBL3138582 — — 1 6.67
CHEMBL3138568 — — 1 6.66
CHEMBL3138564 — — 1 6.62
CHEMBL2062142 — — 1 6.60
CHEMBL3138565 — — 1 6.57
CHEMBL3138554 — — 1 6.55
CHEMBL420483 — — 1 6.47
CHEMBL18861 ZD-6169 — 1 6.41
CHEMBL11684 (-)-CROMAKALIM — 1 6.37
CHEMBL321982 — — 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3138587 — EC50 = 21.88 nM 7.66
CHEMBL3138549 — EC50 = 25.7 nM 7.59
CHEMBL108586 — EC50 = 27.54 nM 7.56
CHEMBL3138545 — EC50 = 28.18 nM 7.55
CHEMBL3138586 — EC50 = 33.11 nM 7.48
CHEMBL3138561 — EC50 = 38.02 nM 7.42
CHEMBL3138553 — EC50 = 43.65 nM 7.36
CHEMBL11458 — EC50 = 44.67 nM 7.35
CHEMBL3138560 — EC50 = 52.48 nM 7.28
CHEMBL3138606 — EC50 = 53.7 nM 7.27
CHEMBL3138596 — EC50 = 54.95 nM 7.26
CHEMBL3138577 — EC50 = 83.18 nM 7.08
CHEMBL3138611 — EC50 = 107.15 nM 6.97
CHEMBL3138607 — EC50 = 123.03 nM 6.91
CHEMBL3138581 — EC50 = 138.04 nM 6.86
CHEMBL3138592 — EC50 = 154.88 nM 6.81
CHEMBL3138548 — EC50 = 181.97 nM 6.74
CHEMBL3138588 — EC50 = 208.93 nM 6.68
CHEMBL3138555 — EC50 = 213.8 nM 6.67
CHEMBL324190 — EC50 = 213.8 nM 6.67
CHEMBL3138582 — EC50 = 213.8 nM 6.67
CHEMBL3138568 — EC50 = 218.78 nM 6.66
CHEMBL3138564 — EC50 = 239.88 nM 6.62
CHEMBL2062142 — EC50 = 251.19 nM 6.60
CHEMBL3138565 — EC50 = 269.15 nM 6.57
CHEMBL3138554 — EC50 = 281.84 nM 6.55
CHEMBL420483 — EC50 = 338.84 nM 6.47
CHEMBL18861 ZD-6169 EC50 = 389.05 nM 6.41
CHEMBL11684 (-)-CROMAKALIM EC50 = 426.58 nM 6.37
CHEMBL321982 — EC50 = 446.68 nM 6.35
CHEMBL3138604 — EC50 = 467.74 nM 6.33
CHEMBL3138594 — EC50 = 501.19 nM 6.30
CHEMBL3138591 — EC50 = 575.44 nM 6.24
CHEMBL3138603 — EC50 = 575.44 nM 6.24
CHEMBL2112479 — EC50 = 630.96 nM 6.20
CHEMBL3138572 — EC50 = 741.31 nM 6.13
CHEMBL3138580 — EC50 = 1047.13 nM 5.98
CHEMBL3138561 — EC50 = 1202.26 nM 5.92
CHEMBL3138605 — EC50 = 1318.26 nM 5.88
CHEMBL3138570 — EC50 = 1348.96 nM 5.87
CHEMBL3138589 — EC50 = 1513.56 nM 5.82
CHEMBL109159 — EC50 = 1819.7 nM 5.74
CHEMBL3138598 — EC50 = 1862.09 nM 5.73
CHEMBL3138567 — EC50 = 2041.74 nM 5.69
CHEMBL3138597 — EC50 = 2238.72 nM 5.65
CHEMBL3138584 — EC50 = 2290.87 nM 5.64
CHEMBL3138556 — EC50 = 2398.83 nM 5.62
CHEMBL3138583 — EC50 = 2570.4 nM 5.59
CHEMBL3138547 — EC50 = 2818.38 nM 5.55
CHEMBL3138552 — EC50 = 3162.28 nM 5.50