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Assay Detail

CHEMBL965360

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

Binding
Binding affinity to batrachotoxinin-sensitive rat brain sodium channel
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.
McAtee JJ, Dodson JW, Dowdell SE, Erhard K, Girard GR, Goodman KB, Hilfiker MA, Jin J, Sehon CA, Sha D, Shi D, Wang F, Wang GZ, Wang N, Wang Y, Viet AQ, Yuan CC, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Douglas SA, Neeb MJ.
Bioorg Med Chem Lett (2008) 18 : 3716 -3719
PubMed 18524591 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 5.00 5.92
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL488642 1 5.92
CHEMBL488470 1 5.70
CHEMBL254356 1 5.60
CHEMBL453075 1 5.11
CHEMBL452808 1 5.03
CHEMBL453074 1 4.95
CHEMBL453067 1 4.77
CHEMBL453329 1 4.66
CHEMBL453587 1 4.66
CHEMBL449192 1 4.52
CHEMBL507691 1 4.52
CHEMBL499582 1 4.52
CHEMBL452298 1 -
CHEMBL527199 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL488642 Ki = 1200.0 nM 5.92
CHEMBL488470 Ki = 2000.0 nM 5.70
CHEMBL254356 Ki = 2500.0 nM 5.60
CHEMBL453075 Ki = 7700.0 nM 5.11
CHEMBL452808 Ki = 9400.0 nM 5.03
CHEMBL453074 Ki = 11130.0 nM 4.95
CHEMBL453067 Ki = 17000.0 nM 4.77
CHEMBL453329 Ki = 22000.0 nM 4.66
CHEMBL453587 Ki = 22000.0 nM 4.66
CHEMBL449192 Ki = 30000.0 nM 4.52
CHEMBL507691 Ki = 30000.0 nM 4.52
CHEMBL499582 Ki = 30000.0 nM 4.52
CHEMBL452298 Ki > 300000.0 nM -
CHEMBL527199 Activity - -