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Assay Detail

CHEMBL779563

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Functional
In vitro inhibitory concentration that relaxed KCL induced contraction in rat detrusor strip by 50%
ChEMBL ↗
77
Total Activities
77
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Expert

Target

Rattus norvegicus (CHEMBL376) ↗
Type ORGANISM
Organism Rattus norvegicus

Publication

Design and SAR of novel potassium channel openers targeted for urge urinary incontinence. 2. Selective and potent benzylamino cyclobutenediones.
Gilbert AM, Antane MM, Argentieri TM, Butera JA, Francisco GD, Freeden C, Gundersen EG, Graceffa RF, Herbst D, Hirth BH, Lennox JR, McFarlane G, Norton NW, Quagliato D, Sheldon JH, Warga D, Wojdan A, Woods M.
J Med Chem (2000) 43 : 1203 -1214
PubMed 10737753 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 77 5.91 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279392 CELIKALIM — 1 7.52
CHEMBL2062142 — — 1 7.05
CHEMBL2062143 — — 1 7.00
CHEMBL19999 — — 1 6.96
CHEMBL19105 — — 1 6.89
CHEMBL19558 — — 1 6.85
CHEMBL278369 — — 1 6.80
CHEMBL277719 — — 1 6.75
CHEMBL19799 — — 1 6.70
CHEMBL20352 — — 1 6.68
CHEMBL19446 — — 1 6.66
CHEMBL19818 — — 1 6.66
CHEMBL19605 — — 1 6.62
CHEMBL417098 — — 1 6.58
CHEMBL20578 — — 1 6.57
CHEMBL278370 — — 1 6.57
CHEMBL281629 — — 1 6.57
CHEMBL20052 — — 1 6.55
CHEMBL19398 — — 1 6.54
CHEMBL283581 — — 1 6.51
CHEMBL19556 — — 1 6.47
CHEMBL278827 — — 1 6.44
CHEMBL20101 — — 1 6.28
CHEMBL442144 — — 1 6.20
CHEMBL19879 — — 1 6.12
CHEMBL20179 — — 1 6.08
CHEMBL278829 — — 1 6.06
CHEMBL18861 ZD-6169 — 1 6.03
CHEMBL19477 — — 1 5.96
CHEMBL281628 — — 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279392 CELIKALIM IC50 = 30.0 nM 7.52
CHEMBL2062142 — IC50 = 90.0 nM 7.05
CHEMBL2062143 — IC50 = 100.0 nM 7.00
CHEMBL19999 — IC50 = 110.0 nM 6.96
CHEMBL19105 — IC50 = 130.0 nM 6.89
CHEMBL19558 — IC50 = 140.0 nM 6.85
CHEMBL278369 — IC50 = 160.0 nM 6.80
CHEMBL277719 — IC50 = 180.0 nM 6.75
CHEMBL19799 — IC50 = 200.0 nM 6.70
CHEMBL20352 — IC50 = 210.0 nM 6.68
CHEMBL19446 — IC50 = 220.0 nM 6.66
CHEMBL19818 — IC50 = 220.0 nM 6.66
CHEMBL19605 — IC50 = 240.0 nM 6.62
CHEMBL417098 — IC50 = 260.0 nM 6.58
CHEMBL281629 — IC50 = 270.0 nM 6.57
CHEMBL278370 — IC50 = 270.0 nM 6.57
CHEMBL20578 — IC50 = 270.0 nM 6.57
CHEMBL20052 — IC50 = 280.0 nM 6.55
CHEMBL19398 — IC50 = 290.0 nM 6.54
CHEMBL283581 — IC50 = 310.0 nM 6.51
CHEMBL19556 — IC50 = 340.0 nM 6.47
CHEMBL278827 — IC50 = 360.0 nM 6.44
CHEMBL20101 — IC50 = 530.0 nM 6.28
CHEMBL442144 — IC50 = 630.0 nM 6.20
CHEMBL19879 — IC50 = 750.0 nM 6.12
CHEMBL20179 — IC50 = 830.0 nM 6.08
CHEMBL278829 — IC50 = 870.0 nM 6.06
CHEMBL18861 ZD-6169 IC50 = 930.0 nM 6.03
CHEMBL19477 — IC50 = 1100.0 nM 5.96
CHEMBL281628 — IC50 = 1100.0 nM 5.96
CHEMBL277842 — IC50 = 1100.0 nM 5.96
CHEMBL19620 — IC50 = 1200.0 nM 5.92
CHEMBL277892 — IC50 = 1300.0 nM 5.89
CHEMBL278546 — IC50 = 1300.0 nM 5.89
CHEMBL20265 — IC50 = 1400.0 nM 5.85
CHEMBL19829 — IC50 = 1500.0 nM 5.82
CHEMBL20288 — IC50 = 1500.0 nM 5.82
CHEMBL19694 — IC50 = 1600.0 nM 5.80
CHEMBL20041 — IC50 = 1700.0 nM 5.77
CHEMBL19858 — IC50 = 1900.0 nM 5.72
CHEMBL19516 — IC50 = 2000.0 nM 5.70
CHEMBL279318 — IC50 = 2100.0 nM 5.68
CHEMBL20018 — IC50 = 2100.0 nM 5.68
CHEMBL2079657 — IC50 = 2200.0 nM 5.66
CHEMBL441956 — IC50 = 2400.0 nM 5.62
CHEMBL20285 — IC50 = 2600.0 nM 5.58
CHEMBL20186 — IC50 = 3000.0 nM 5.52
CHEMBL19909 — IC50 = 3400.0 nM 5.47
CHEMBL19775 — IC50 = 3900.0 nM 5.41
CHEMBL2079580 — IC50 = 4000.0 nM 5.40