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Assay Detail

CHEMBL762567

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

Functional
Relaxing effect determined by measuring inhibition of acetylcholine-induced contractions in pig coronary arteries.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Sus scrofa
Confidence 1 — Organism
Curated By Expert

Target

Sus scrofa (CHEMBL613488)
Type ORGANISM
Organism Sus scrofa

Publication

3-Methyl-2H-1-benzopyran potassium channel activators.
Gericke R, Harting J, Lues I, Schittenhelm C.
J Med Chem (1991) 34 : 3074 -3085
PubMed 1920358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.24 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL106121 1 8.40
CHEMBL104552 1 8.22
CHEMBL108107 1 8.15
CHEMBL322249 1 7.70
CHEMBL317641 1 7.70
CHEMBL316977 1 7.70
CHEMBL318737 1 7.52
CHEMBL327249 1 7.30
CHEMBL12552 BIMAKALIM 2.0 1 7.30
CHEMBL318520 EMAKALIM 2.0 1 6.52
CHEMBL266381 1 6.16
CHEMBL49035 CROMAKALIM 2.0 1 6.16
CHEMBL106594 1 5.40
CHEMBL325775 1 5.30
CHEMBL105481 1 5.22
CHEMBL105852 1 4.70
CHEMBL106390 1 4.70
CHEMBL106179 1 4.40
CHEMBL106600 1 4.30
CHEMBL320905 1 4.10
CHEMBL104635 1 4.00
CHEMBL406508 1 -
CHEMBL105038 1 -
CHEMBL319428 1 -
CHEMBL102475 1 -
CHEMBL104860 1 -
CHEMBL106122 1 -
CHEMBL105799 1 -
CHEMBL101688 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL106121 IC50 = 4.0 nM 8.40
CHEMBL104552 IC50 = 6.0 nM 8.22
CHEMBL108107 IC50 = 7.0 nM 8.15
CHEMBL322249 IC50 = 20.0 nM 7.70
CHEMBL317641 IC50 = 20.0 nM 7.70
CHEMBL316977 IC50 = 20.0 nM 7.70
CHEMBL318737 IC50 = 30.0 nM 7.52
CHEMBL327249 IC50 = 50.0 nM 7.30
CHEMBL12552 BIMAKALIM IC50 = 50.0 nM 7.30
CHEMBL318520 EMAKALIM IC50 = 300.0 nM 6.52
CHEMBL266381 IC50 = 700.0 nM 6.16
CHEMBL49035 CROMAKALIM IC50 = 700.0 nM 6.16
CHEMBL106594 IC50 = 4000.0 nM 5.40
CHEMBL325775 IC50 = 5000.0 nM 5.30
CHEMBL105481 IC50 = 6000.0 nM 5.22
CHEMBL105852 IC50 = 20000.0 nM 4.70
CHEMBL106390 IC50 = 20000.0 nM 4.70
CHEMBL106179 IC50 = 40000.0 nM 4.40
CHEMBL106600 IC50 = 50000.0 nM 4.30
CHEMBL320905 IC50 = 80000.0 nM 4.10
CHEMBL104635 IC50 = 100000.0 nM 4.00
CHEMBL406508 IC50 > 100000.0 nM -
CHEMBL105038 IC50 > 100000.0 nM -
CHEMBL319428 IC50 > 100000.0 nM -
CHEMBL102475 IC50 > 100000.0 nM -
CHEMBL104860 IC50 > 100000.0 nM -
CHEMBL106122 IC50 > 100000.0 nM -
CHEMBL105799 IC50 > 100000.0 nM -
CHEMBL101688 IC50 > 100000.0 nM -