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Assay Detail

CHEMBL700928

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

Functional
Maximum activation of human KATP (SUR1/Kir6.2) channel expressed in Xenopus oocytes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Oocyte
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Sulfonylurea receptor 1, Kir6.2 (CHEMBL2096972)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

3-trifluoromethyl-4-nitro-5-arylpyrazoles are novel K(ATP) channel agonists.
Peat AJ, Townsend C, Craig McKay M, Garrido D, Terry CM, Wilson JL, Thomson SA.
Bioorg Med Chem Lett (2004) 14 : 813 -816
PubMed 14741296 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 5.85 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL354554 1 7.16
CHEMBL353185 1 6.27
CHEMBL422377 1 6.16
CHEMBL169038 1 5.94
CHEMBL181 DIAZOXIDE 4.0 1 5.06
CHEMBL167508 1 4.52
CHEMBL168681 1 -
CHEMBL354344 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL354554 EC50 = 70.0 nM 7.16
CHEMBL353185 EC50 = 540.0 nM 6.27
CHEMBL422377 EC50 = 700.0 nM 6.16
CHEMBL169038 EC50 = 1150.0 nM 5.94
CHEMBL181 DIAZOXIDE EC50 = 8800.0 nM 5.06
CHEMBL167508 EC50 = 30000.0 nM 4.52
CHEMBL168681 EC50 > 30000.0 nM -
CHEMBL354344 EC50 > 30000.0 nM -