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Assay Detail

CHEMBL908895

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

Functional
Ability to open human urinary bladder Kir6.2 channel containing SUR2B in Ltk cells by FLIPR assay
ChEMBL ↗
157
Total Activities
78
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Ltk
Confidence 7 — Homologous single protein target
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 141 6.66 9.04
Activity 16 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL426334 — — 3 9.04
CHEMBL218564 — — 3 9.00
CHEMBL214561 — — 1 8.93
CHEMBL413532 — — 1 8.74
CHEMBL217810 — — 1 8.56
CHEMBL384564 — — 3 8.41
CHEMBL217847 — — 1 8.22
CHEMBL386363 — — 1 8.01
CHEMBL386119 — — 3 7.85
CHEMBL265269 — — 1 7.84
CHEMBL216766 — — 1 7.77
CHEMBL216284 — — 1 7.74
CHEMBL216546 — — 3 7.64
CHEMBL386582 — — 3 7.62
CHEMBL261996 — — 1 7.57
CHEMBL426160 — — 3 7.57
CHEMBL214841 — — 5 7.56
CHEMBL320983 — — 1 7.56
CHEMBL384576 — — 1 7.56
CHEMBL386323 — — 1 7.53
CHEMBL217511 — — 2 7.43
CHEMBL11458 — — 1 7.28
CHEMBL412838 — — 1 7.25
CHEMBL3138600 — — 1 7.25
CHEMBL2112487 — — 1 7.20
CHEMBL215996 — — 3 7.19
CHEMBL214566 — — 4 7.17
CHEMBL424726 — — 1 7.14
CHEMBL386126 — — 5 7.14
CHEMBL215375 — — 5 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL426334 — EC50 = 0.912 nM 9.04
CHEMBL218564 — EC50 = 1.0 nM 9.00
CHEMBL214561 — EC50 = 1.175 nM 8.93
CHEMBL413532 — EC50 = 1.82 nM 8.74
CHEMBL217810 — EC50 = 2.754 nM 8.56
CHEMBL218564 — EC50 = 3.715 nM 8.43
CHEMBL384564 — EC50 = 3.89 nM 8.41
CHEMBL218564 — EC50 = 5.129 nM 8.29
CHEMBL426334 — EC50 = 5.495 nM 8.26
CHEMBL217847 — EC50 = 6.026 nM 8.22
CHEMBL386363 — EC50 = 9.772 nM 8.01
CHEMBL386119 — EC50 = 14.13 nM 7.85
CHEMBL265269 — EC50 = 14.45 nM 7.84
CHEMBL216766 — EC50 = 16.98 nM 7.77
CHEMBL216284 — EC50 = 18.2 nM 7.74
CHEMBL386119 — EC50 = 19.95 nM 7.70
CHEMBL216546 — EC50 = 22.91 nM 7.64
CHEMBL216546 — EC50 = 22.91 nM 7.64
CHEMBL386582 — EC50 = 23.99 nM 7.62
CHEMBL426160 — EC50 = 26.92 nM 7.57
CHEMBL261996 — EC50 = 26.92 nM 7.57
CHEMBL386582 — EC50 = 26.92 nM 7.57
CHEMBL214841 — EC50 = 27.54 nM 7.56
CHEMBL384576 — EC50 = 27.54 nM 7.56
CHEMBL320983 — EC50 = 27.54 nM 7.56
CHEMBL386323 — EC50 = 29.51 nM 7.53
CHEMBL384564 — EC50 = 35.48 nM 7.45
CHEMBL217511 — EC50 = 37.15 nM 7.43
CHEMBL217511 — EC50 = 45.71 nM 7.34
CHEMBL426334 — EC50 = 51.29 nM 7.29
CHEMBL11458 — EC50 = 52.48 nM 7.28
CHEMBL412838 — EC50 = 56.23 nM 7.25
CHEMBL3138600 — EC50 = 56.23 nM 7.25
CHEMBL2112487 — EC50 = 63.1 nM 7.20
CHEMBL215996 — EC50 = 64.57 nM 7.19
CHEMBL214566 — EC50 = 67.61 nM 7.17
CHEMBL386126 — EC50 = 72.44 nM 7.14
CHEMBL424726 — EC50 = 72.44 nM 7.14
CHEMBL426160 — EC50 = 75.86 nM 7.12
CHEMBL214566 — EC50 = 91.2 nM 7.04
CHEMBL215375 — EC50 = 95.5 nM 7.02
CHEMBL384078 — EC50 = 102.33 nM 6.99
CHEMBL385908 — EC50 = 102.33 nM 6.99
CHEMBL216256 — EC50 = 104.71 nM 6.98
CHEMBL217696 — EC50 = 120.23 nM 6.92
CHEMBL215026 — EC50 = 125.89 nM 6.90
CHEMBL3138574 — EC50 = 134.9 nM 6.87
CHEMBL386136 — EC50 = 134.9 nM 6.87
CHEMBL384564 — EC50 = 144.54 nM 6.84
CHEMBL215124 — EC50 = 151.36 nM 6.82