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Assay Detail

CHEMBL908308

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

Functional
Activity against pig bladder KATP channel opening assessed as ability to relax field-stimulated pig detrusor
30
Total Activities
22
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Sus scrofa
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Sulfonylurea receptor 2, Kir6.2 (CHEMBL2095198)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Effects of substitution on 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a dihydropyridine ATP-sensitive potassium channel opener.
Altenbach RJ, Brune ME, Buckner SA, Coghlan MJ, Daza AV, Fabiyi A, Gopalakrishnan M, Henry RF, Khilevich A, Kort ME, Milicic I, Scott VE, Smith JC, Whiteaker KL, Carroll WA.
J Med Chem (2006) 49 : 6869 -6887
PubMed 17154517 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 6.23 7.45
Activity 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL426334 1 7.45
CHEMBL11458 1 7.07
CHEMBL386228 1 6.99
CHEMBL320983 1 6.90
CHEMBL384576 1 6.89
CHEMBL214566 1 6.89
CHEMBL217511 1 6.67
CHEMBL426160 1 6.64
CHEMBL11684 (-)-CROMAKALIM 1 6.59
CHEMBL215375 4 6.55
CHEMBL214841 3 6.29
CHEMBL2112487 1 6.23
CHEMBL2062142 1 6.17
CHEMBL384078 3 6.05
CHEMBL215681 2 6.05
CHEMBL214616 1 5.92
CHEMBL386628 1 5.89
CHEMBL386843 1 5.78
CHEMBL424909 1 5.69
CHEMBL216256 1 5.64
CHEMBL18861 ZD-6169 1 5.56
CHEMBL387063 1 4.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL426334 EC50 = 35.48 nM 7.45
CHEMBL11458 EC50 = 85.11 nM 7.07
CHEMBL386228 EC50 = 102.33 nM 6.99
CHEMBL320983 EC50 = 125.89 nM 6.90
CHEMBL384576 EC50 = 128.82 nM 6.89
CHEMBL214566 EC50 = 128.82 nM 6.89
CHEMBL217511 EC50 = 213.8 nM 6.67
CHEMBL426160 EC50 = 229.09 nM 6.64
CHEMBL11684 (-)-CROMAKALIM EC50 = 257.04 nM 6.59
CHEMBL215375 EC50 = 281.84 nM 6.55
CHEMBL215375 EC50 = 489.78 nM 6.31
CHEMBL214841 EC50 = 512.86 nM 6.29
CHEMBL2112487 EC50 = 588.84 nM 6.23
CHEMBL2062142 EC50 = 676.08 nM 6.17
CHEMBL214841 EC50 = 794.33 nM 6.10
CHEMBL384078 EC50 = 891.25 nM 6.05
CHEMBL215681 EC50 = 891.25 nM 6.05
CHEMBL384078 EC50 = 954.99 nM 6.02
CHEMBL214616 EC50 = 1202.26 nM 5.92
CHEMBL386628 EC50 = 1288.25 nM 5.89
CHEMBL386843 EC50 = 1659.59 nM 5.78
CHEMBL424909 EC50 = 2041.74 nM 5.69
CHEMBL216256 EC50 = 2290.87 nM 5.64
CHEMBL215681 EC50 = 2691.53 nM 5.57
CHEMBL18861 ZD-6169 EC50 = 2754.23 nM 5.56
CHEMBL215375 EC50 = 2951.21 nM 5.53
CHEMBL387063 EC50 = 13489.63 nM 4.87
CHEMBL215375 Activity - -
CHEMBL214841 Activity - -
CHEMBL384078 Activity - -