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Assay Detail

CHEMBL779564

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Functional
In vitro inhibitory concentration that relaxes KCL induced contraction in rat detrusor strips by 50%
ChEMBL ↗
78
Total Activities
76
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. 1. N-Cyanoguanidine bioisosteres possessing in vivo bladder selectivity.
Butera JA, Antane MM, Antane SA, Argentieri TM, Freeden C, Graceffa RF, Hirth BH, Jenkins D, Lennox JR, Matelan E, Norton NW, Quagliato D, Sheldon JH, Spinelli W, Warga D, Wojdan A, Woods M.
J Med Chem (2000) 43 : 1187 -1202
PubMed 10737752 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 78 5.76 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279392 CELIKALIM — 1 7.52
CHEMBL18931 — — 1 7.39
CHEMBL2079574 — — 1 7.25
CHEMBL278485 — — 1 7.12
CHEMBL2062142 — — 1 7.05
CHEMBL19169 — — 1 6.72
CHEMBL276328 — — 1 6.54
CHEMBL18859 — — 1 6.47
CHEMBL2079648 — — 2 6.43
CHEMBL19265 — — 1 6.28
CHEMBL279150 — — 1 6.25
CHEMBL18951 — — 1 6.20
CHEMBL1159 PINACIDIL ANHYDROUS 4.0 1 6.20
CHEMBL275401 — — 1 6.17
CHEMBL19110 — — 1 6.13
CHEMBL18861 ZD-6169 — 1 6.03
CHEMBL273362 — — 1 5.97
CHEMBL278694 — — 1 5.90
CHEMBL18519 — — 1 5.87
CHEMBL1907923 — — 1 5.78
CHEMBL19073 — — 1 5.75
CHEMBL19192 — — 1 5.74
CHEMBL1907922 — — 1 5.72
CHEMBL18639 — — 1 5.72
CHEMBL19555 — — 1 5.71
CHEMBL19025 — — 1 5.68
CHEMBL18934 — — 1 5.62
CHEMBL277365 — — 1 5.59
CHEMBL2079573 — — 1 5.58
CHEMBL19088 — — 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279392 CELIKALIM IC50 = 30.0 nM 7.52
CHEMBL18931 — IC50 = 41.0 nM 7.39
CHEMBL2079574 — IC50 = 56.0 nM 7.25
CHEMBL278485 — IC50 = 75.0 nM 7.12
CHEMBL2062142 — IC50 = 90.0 nM 7.05
CHEMBL19169 — IC50 = 190.0 nM 6.72
CHEMBL276328 — IC50 = 290.0 nM 6.54
CHEMBL18859 — IC50 = 340.0 nM 6.47
CHEMBL2079648 — IC50 = 370.0 nM 6.43
CHEMBL19265 — IC50 = 520.0 nM 6.28
CHEMBL279150 — IC50 = 560.0 nM 6.25
CHEMBL18951 — IC50 = 630.0 nM 6.20
CHEMBL1159 PINACIDIL ANHYDROUS IC50 = 630.0 nM 6.20
CHEMBL275401 — IC50 = 670.0 nM 6.17
CHEMBL19110 — IC50 = 740.0 nM 6.13
CHEMBL18861 ZD-6169 IC50 = 930.0 nM 6.03
CHEMBL273362 — IC50 = 1080.0 nM 5.97
CHEMBL278694 — IC50 = 1260.0 nM 5.90
CHEMBL18519 — IC50 = 1360.0 nM 5.87
CHEMBL1907923 — IC50 = 1680.0 nM 5.78
CHEMBL19073 — IC50 = 1770.0 nM 5.75
CHEMBL19192 — IC50 = 1840.0 nM 5.74
CHEMBL18639 — IC50 = 1900.0 nM 5.72
CHEMBL1907922 — IC50 = 1900.0 nM 5.72
CHEMBL19555 — IC50 = 1950.0 nM 5.71
CHEMBL19025 — IC50 = 2100.0 nM 5.68
CHEMBL18934 — IC50 = 2400.0 nM 5.62
CHEMBL277365 — IC50 = 2560.0 nM 5.59
CHEMBL2079573 — IC50 = 2600.0 nM 5.58
CHEMBL19088 — IC50 = 2800.0 nM 5.55
CHEMBL283161 — IC50 = 3050.0 nM 5.52
CHEMBL417636 — IC50 = 3340.0 nM 5.48
CHEMBL19077 — IC50 = 3350.0 nM 5.47
CHEMBL19133 — IC50 = 4000.0 nM 5.40
CHEMBL19420 — IC50 = 4300.0 nM 5.37
CHEMBL18971 — IC50 = 4600.0 nM 5.34
CHEMBL275166 — IC50 = 4780.0 nM 5.32
CHEMBL18900 — IC50 = 5400.0 nM 5.27
CHEMBL19253 — IC50 = 6050.0 nM 5.22
CHEMBL18482 — IC50 = 8100.0 nM 5.09
CHEMBL444260 — IC50 = 11500.0 nM 4.94
CHEMBL278299 — IC50 = 11740.0 nM 4.93
CHEMBL19089 — IC50 = 13700.0 nM 4.86
CHEMBL19196 — IC50 = 14300.0 nM 4.84
CHEMBL19245 — IC50 = 17600.0 nM 4.75
CHEMBL19257 — IC50 = 21200.0 nM 4.67
CHEMBL2079572 — IC50 = 22500.0 nM 4.65
CHEMBL19492 — IC50 = 23100.0 nM 4.64
CHEMBL2079648 — IC50 = 24300.0 nM 4.61
CHEMBL19122 — IC50 > 30000.0 nM -