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

CHEMBL1116628

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

Binding
Blocking of rat Voltage-dependent L-type calcium channel alpha1c/alpha2delta-1/beta1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Scaffold-based design and synthesis of potent N-type calcium channel blockers.
Zamponi GW, Feng ZP, Zhang L, Pajouhesh H, Ding Y, Belardetti F, Pajouhesh H, Dolphin D, Mitscher LA, Snutch TP.
Bioorg Med Chem Lett (2009) 19 : 6467 -6472
PubMed 19815411 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.20 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1087660 1 6.92
CHEMBL29188 LOMERIZINE 2.0 1 6.82
CHEMBL1087275 1 6.60
CHEMBL30008 FLUNARIZINE 2.0 1 6.51
CHEMBL1088309 2 6.48
CHEMBL1088610 1 6.13
CHEMBL1087237 1 6.08
CHEMBL599217 1 5.74
CHEMBL1086621 1 5.55
CHEMBL604710 Z160 2.0 1 4.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1087660 IC50 = 120.0 nM 6.92
CHEMBL29188 LOMERIZINE IC50 = 150.0 nM 6.82
CHEMBL1087275 IC50 = 250.0 nM 6.60
CHEMBL30008 FLUNARIZINE IC50 = 310.0 nM 6.51
CHEMBL1088309 IC50 = 330.0 nM 6.48
CHEMBL1088309 IC50 = 390.0 nM 6.41
CHEMBL1088610 IC50 = 740.0 nM 6.13
CHEMBL1087237 IC50 = 830.0 nM 6.08
CHEMBL599217 IC50 = 1840.0 nM 5.74
CHEMBL1086621 IC50 = 2840.0 nM 5.55
CHEMBL604710 Z160 IC50 = 12200.0 nM 4.91