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Assay Detail

CHEMBL921653

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

Binding
Binding affinity at batrachotoxinin sensitive Sodium channel in rat brain
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Development of potent and selective small-molecule human Urotensin-II antagonists.
McAtee JJ, Dodson JW, Dowdell SE, Girard GR, Goodman KB, Hilfiker MA, Sehon CA, Sha D, Wang GZ, Wang N, Viet AQ, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Yuan CC, Douglas SA, Neeb MJ.
Bioorg Med Chem Lett (2008) 18 : 3500 -3503
PubMed 18502123 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 5.84 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL257150 1 6.82
CHEMBL255462 1 6.48
CHEMBL257171 1 6.41
CHEMBL255509 1 6.17
CHEMBL404289 1 6.14
CHEMBL256989 1 6.03
CHEMBL256937 1 6.02
CHEMBL402520 1 5.89
CHEMBL257415 1 5.85
CHEMBL402805 1 5.80
CHEMBL257767 1 5.80
CHEMBL254356 1 5.60
CHEMBL402813 1 5.50
CHEMBL255460 1 5.46
CHEMBL258251 1 5.40
CHEMBL256721 1 5.16
CHEMBL256988 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL257150 Ki = 150.0 nM 6.82
CHEMBL255462 Ki = 330.0 nM 6.48
CHEMBL257171 Ki = 390.0 nM 6.41
CHEMBL255509 Ki = 680.0 nM 6.17
CHEMBL404289 Ki = 730.0 nM 6.14
CHEMBL256989 Ki = 930.0 nM 6.03
CHEMBL256937 Ki = 960.0 nM 6.02
CHEMBL402520 Ki = 1300.0 nM 5.89
CHEMBL257415 Ki = 1400.0 nM 5.85
CHEMBL402805 Ki = 1600.0 nM 5.80
CHEMBL257767 Ki = 1600.0 nM 5.80
CHEMBL254356 Ki = 2500.0 nM 5.60
CHEMBL402813 Ki = 3200.0 nM 5.50
CHEMBL255460 Ki = 3500.0 nM 5.46
CHEMBL258251 Ki = 4000.0 nM 5.40
CHEMBL256721 Ki = 6900.0 nM 5.16
CHEMBL256988 Ki = 18000.0 nM 4.75