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Assay Detail

CHEMBL699661

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

Functional
K-ATP activity in terms of stable twitch response through field-stimulated landrace pig detrusor assay
26
Total Activities
25
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Sus scrofa
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
Log EC50 19 - -
EC50 7 6.11 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3138573 1 7.17
CHEMBL3392139 2 6.61
CHEMBL3392140 1 6.26
CHEMBL106033 1 6.01
CHEMBL110511 1 5.93
CHEMBL108816 1 5.63
CHEMBL323460 1 5.16
CHEMBL108723 1 -
CHEMBL323787 1 -
CHEMBL108440 1 -
CHEMBL109196 1 -
CHEMBL325339 1 -
CHEMBL109994 1 -
CHEMBL108658 1 -
CHEMBL108251 1 -
CHEMBL322931 1 -
CHEMBL107933 1 -
CHEMBL322507 1 -
CHEMBL321210 1 -
CHEMBL3138579 1 -
CHEMBL320337 1 -
CHEMBL324618 1 -
CHEMBL108400 1 -
CHEMBL111297 1 -
CHEMBL109412 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3138573 EC50 = 67.61 nM 7.17
CHEMBL3392139 EC50 = 245.47 nM 6.61
CHEMBL3392140 EC50 = 549.54 nM 6.26
CHEMBL106033 EC50 = 977.24 nM 6.01
CHEMBL110511 EC50 = 1174.9 nM 5.93
CHEMBL108816 EC50 = 2344.23 nM 5.63
CHEMBL323460 EC50 = 6918.31 nM 5.16
CHEMBL109994 Log EC50 - -
CHEMBL325339 Log EC50 - -
CHEMBL322931 Log EC50 - -
CHEMBL108723 Log EC50 - -
CHEMBL323787 Log EC50 - -
CHEMBL108440 Log EC50 - -
CHEMBL109196 Log EC50 - -
CHEMBL3392139 Log EC50 - -
CHEMBL108658 Log EC50 - -
CHEMBL109412 Log EC50 - -
CHEMBL107933 Log EC50 - -
CHEMBL322507 Log EC50 - -
CHEMBL321210 Log EC50 - -
CHEMBL3138579 Log EC50 - -
CHEMBL320337 Log EC50 - -
CHEMBL324618 Log EC50 - -
CHEMBL108400 Log EC50 - -
CHEMBL108251 Log EC50 - -
CHEMBL111297 Log EC50 - -