Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1068016

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

Binding
Inhibition of L type calcium channel alpha-1c/alpha-2-delta-1/beta-1b expressed in HEK293 cells in presence of -100 mV holding potential by whole-cell patch clamp method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Publication

Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors.
Pajouhesh H, Feng ZP, Ding Y, Zhang L, Pajouhesh H, Morrison JL, Belardetti F, Tringham E, Simonson E, Vanderah TW, Porreca F, Zamponi GW, Mitscher LA, Snutch TP.
Bioorg Med Chem Lett (2010) 20 : 1378 -1383
PubMed 20117000 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.12 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL603465 1 6.21
CHEMBL596942 1 5.99
CHEMBL599217 1 5.74
CHEMBL599402 1 5.37
CHEMBL597788 1 5.18
CHEMBL599404 1 5.07
CHEMBL597783 1 4.96
CHEMBL604710 Z160 2.0 1 4.91
CHEMBL597756 1 4.75
CHEMBL597585 1 4.71
CHEMBL608740 1 4.52
CHEMBL598812 1 4.00
CHEMBL598592 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL603465 IC50 = 610.0 nM 6.21
CHEMBL596942 IC50 = 1030.0 nM 5.99
CHEMBL599217 IC50 = 1840.0 nM 5.74
CHEMBL599402 IC50 = 4300.0 nM 5.37
CHEMBL597788 IC50 = 6600.0 nM 5.18
CHEMBL599404 IC50 = 8500.0 nM 5.07
CHEMBL597783 IC50 = 11000.0 nM 4.96
CHEMBL604710 Z160 IC50 = 12200.0 nM 4.91
CHEMBL597756 IC50 = 17900.0 nM 4.75
CHEMBL597585 IC50 = 19600.0 nM 4.71
CHEMBL608740 IC50 = 30000.0 nM 4.52
CHEMBL598812 IC50 = 100000.0 nM 4.00
CHEMBL598592 IC50 = 106000.0 nM -