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Assay Detail

CHEMBL2154368

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

Functional
Antagonist activity at depolarized T-type calcium channel by FLIPR assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Short-acting T-type calcium channel antagonists significantly modify sleep architecture in rodents.
Yang ZQ, Schlegel KA, Shu Y, Reger TS, Cube R, Mattern C, Coleman PJ, Small J, Hartman GD, Ballard J, Tang C, Kuo Y, Prueksaritanont T, Nuss CE, Doran S, Fox SV, Garson SL, Li Y, Kraus RL, Uebele VN, Taylor AB, Zeng W, Fang W, Chavez-Eng C, Troyer MD, Luk JA, Laethem T, Cook WO, Renger JJ, Barrow JC.
ACS Med Chem Lett (2010) 1 : 504 -509
PubMed 24900239 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.10 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2151144 1 8.43
CHEMBL2151145 1 8.28
CHEMBL2151146 1 8.27
CHEMBL1684954 1 8.03
CHEMBL2151147 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2151144 IC50 = 3.7 nM 8.43
CHEMBL2151145 IC50 = 5.3 nM 8.28
CHEMBL2151146 IC50 = 5.4 nM 8.27
CHEMBL1684954 IC50 = 9.4 nM 8.03
CHEMBL2151147 IC50 = 31.3 nM 7.50