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Assay Detail

CHEMBL799883

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

Functional
Concentration required to cause 50% inhibition of spontaneous activity in rat portal vein
39
Total Activities
37
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

Structure-activity studies of potassium channel opening in pinacidil-type cyanoguanidines, nitroethenediamines, thioureas, and ureas.
Manley PW, Quast U.
J Med Chem (1992) 35 : 2327 -2340
PubMed 1613756 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 6.19 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11458 1 8.70
CHEMBL2115097 2 8.00
CHEMBL75020 1 7.90
CHEMBL2115176 1 7.80
CHEMBL75172 1 7.80
CHEMBL557537 1 7.50
CHEMBL398879 (R)-PINACIDIL 1 7.47
CHEMBL75584 1 7.30
CHEMBL1159 PINACIDIL ANHYDROUS 4.0 1 7.20
CHEMBL2114145 2 7.00
CHEMBL77571 1 7.00
CHEMBL74146 1 6.70
CHEMBL75362 1 6.70
CHEMBL2094045 1 6.50
CHEMBL431391 1 6.50
CHEMBL2093881 1 6.30
CHEMBL251647 (S)-PINACIDIL 1 6.11
CHEMBL75857 1 6.00
CHEMBL77854 1 6.00
CHEMBL307741 1 6.00
CHEMBL74245 1 6.00
CHEMBL2114147 1 5.80
CHEMBL75585 1 5.70
CHEMBL73592 1 5.70
CHEMBL76996 1 5.70
CHEMBL74732 1 5.50
CHEMBL539267 1 5.50
CHEMBL78117 1 5.50
CHEMBL75622 1 5.50
CHEMBL311157 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11458 IC50 = 1.995 nM 8.70
CHEMBL2115097 IC50 = 10.0 nM 8.00
CHEMBL75020 IC50 = 12.59 nM 7.90
CHEMBL75172 IC50 = 15.85 nM 7.80
CHEMBL2115176 IC50 = 15.85 nM 7.80
CHEMBL557537 IC50 = 31.62 nM 7.50
CHEMBL398879 (R)-PINACIDIL IC50 = 33.88 nM 7.47
CHEMBL75584 IC50 = 50.12 nM 7.30
CHEMBL1159 PINACIDIL ANHYDROUS IC50 = 63.1 nM 7.20
CHEMBL77571 IC50 = 100.0 nM 7.00
CHEMBL2114145 IC50 = 100.0 nM 7.00
CHEMBL74146 IC50 = 199.53 nM 6.70
CHEMBL75362 IC50 = 199.53 nM 6.70
CHEMBL2094045 IC50 = 316.23 nM 6.50
CHEMBL431391 IC50 = 316.23 nM 6.50
CHEMBL2093881 IC50 = 501.19 nM 6.30
CHEMBL251647 (S)-PINACIDIL IC50 = 776.25 nM 6.11
CHEMBL74245 IC50 = 1000.0 nM 6.00
CHEMBL307741 IC50 = 1000.0 nM 6.00
CHEMBL77854 IC50 = 1000.0 nM 6.00
CHEMBL75857 IC50 = 1000.0 nM 6.00
CHEMBL2115097 IC50 = 1000.0 nM 6.00
CHEMBL2114147 IC50 = 1584.89 nM 5.80
CHEMBL75585 IC50 = 1995.26 nM 5.70
CHEMBL76996 IC50 = 1995.26 nM 5.70
CHEMBL73592 IC50 = 1995.26 nM 5.70
CHEMBL78117 IC50 = 3162.28 nM 5.50
CHEMBL75622 IC50 = 3162.28 nM 5.50
CHEMBL74732 IC50 = 3162.28 nM 5.50
CHEMBL539267 IC50 = 3162.28 nM 5.50
CHEMBL311157 IC50 = 5011.87 nM 5.30
CHEMBL2114145 IC50 = 6309.57 nM 5.20
CHEMBL75062 IC50 = 10000.0 nM 5.00
CHEMBL75965 IC50 = 19952.62 nM 4.70
CHEMBL308334 IC50 = 19952.62 nM 4.70
CHEMBL307840 IC50 = 31622.78 nM 4.50
CHEMBL305882 IC50 = 31622.78 nM 4.50
CHEMBL76594 IC50 = 100000.0 nM 4.00
CHEMBL307913 IC50 < 10000.0 nM -