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Assay Detail

CHEMBL4260481

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

Binding
Activation of human Kv7.3/7.5 by patch clamp method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Intermediate

Target

Voltage-gated potassium channel KCNQ3/KCNQ5 (CHEMBL3883311)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Novel KV7 ion channel openers for the treatment of epilepsy and implications for detrusor tissue contraction.
Seefeld MA, Lin H, Holenz J, Downie D, Donovan B, Fu T, Pasikanti K, Zhen W, Cato M, Chaudhary KW, Brady P, Bakshi T, Morrow D, Rajagopal S, Samanta SK, Madhyastha N, Kuppusamy BM, Dougherty RW, Bhamidipati R, Mohd Z, Higgins GA, Chapman M, Rouget C, Lluel P, Matsuoka Y.
Bioorg Med Chem Lett (2018) 28 : 3793 -3797
PubMed 30327146 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.59 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4278049 1 7.10
CHEMBL4288707 1 6.70
CHEMBL4277250 1 6.60
CHEMBL4287894 1 6.44
CHEMBL4287478 1 6.40
CHEMBL1703636 1 6.30
CHEMBL402146 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4278049 EC50 = 80.0 nM 7.10
CHEMBL4288707 EC50 = 200.0 nM 6.70
CHEMBL4277250 EC50 = 250.0 nM 6.60
CHEMBL4287894 EC50 = 360.0 nM 6.44
CHEMBL4287478 EC50 = 400.0 nM 6.40
CHEMBL1703636 EC50 = 500.0 nM 6.30
CHEMBL402146 EC50 > 10000.0 nM -