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Assay Detail

CHEMBL3880754

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

Binding
Antagonist activity at rat alpha1B N-type calcium channel expressed in HEK293 cells assessed as 0.067 Hz current frequency dependent channel blocking for 2 mins in presence of Ba2+ by whole-cell patch clamp assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Voltage-dependent N-type calcium channel subunit alpha-1B (CHEMBL5107)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Calcium channel inhibitors comprising benzhydril spaced from piperazine
(2004)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.47 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL597585 1 7.00
CHEMBL3978555 1 6.80
CHEMBL596946 1 6.77
CHEMBL597788 1 6.70
CHEMBL3927466 1 6.67
CHEMBL3939633 1 6.67
CHEMBL3915774 1 6.64
CHEMBL598806 1 6.64
CHEMBL3930176 1 6.54
CHEMBL3949401 1 6.54
CHEMBL3972049 1 6.54
CHEMBL3935114 1 6.52
CHEMBL3967577 1 6.52
CHEMBL606175 1 6.50
CHEMBL599016 1 6.50
CHEMBL599015 1 6.49
CHEMBL3896085 1 6.47
CHEMBL599832 1 6.46
CHEMBL598603 1 6.44
CHEMBL3927871 1 6.43
CHEMBL3942862 1 6.36
CHEMBL597970 1 6.31
CHEMBL598990 1 6.27
CHEMBL3918151 1 6.26
CHEMBL597969 1 6.22
CHEMBL3950908 1 6.15
CHEMBL3916031 1 6.13
CHEMBL3956949 1 6.07
CHEMBL589285 1 5.96
CHEMBL3956201 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL597585 IC50 = 100.0 nM 7.00
CHEMBL3978555 IC50 = 160.0 nM 6.80
CHEMBL596946 IC50 = 170.0 nM 6.77
CHEMBL597788 IC50 = 200.0 nM 6.70
CHEMBL3927466 IC50 = 213.0 nM 6.67
CHEMBL3939633 IC50 = 213.0 nM 6.67
CHEMBL3915774 IC50 = 230.0 nM 6.64
CHEMBL598806 IC50 = 230.0 nM 6.64
CHEMBL3930176 IC50 = 291.0 nM 6.54
CHEMBL3949401 IC50 = 286.0 nM 6.54
CHEMBL3972049 IC50 = 290.0 nM 6.54
CHEMBL3935114 IC50 = 300.0 nM 6.52
CHEMBL3967577 IC50 = 300.0 nM 6.52
CHEMBL606175 IC50 = 320.0 nM 6.50
CHEMBL599016 IC50 = 320.0 nM 6.50
CHEMBL599015 IC50 = 324.0 nM 6.49
CHEMBL3896085 IC50 = 340.0 nM 6.47
CHEMBL599832 IC50 = 348.0 nM 6.46
CHEMBL598603 IC50 = 360.0 nM 6.44
CHEMBL3927871 IC50 = 370.0 nM 6.43
CHEMBL3942862 IC50 = 437.0 nM 6.36
CHEMBL597970 IC50 = 490.0 nM 6.31
CHEMBL598990 IC50 = 538.0 nM 6.27
CHEMBL3918151 IC50 = 550.0 nM 6.26
CHEMBL597969 IC50 = 600.0 nM 6.22
CHEMBL3950908 IC50 = 710.0 nM 6.15
CHEMBL3916031 IC50 = 737.0 nM 6.13
CHEMBL3956949 IC50 = 854.0 nM 6.07
CHEMBL589285 IC50 = 1090.0 nM 5.96
CHEMBL3956201 IC50 > 1000.0 nM -
CHEMBL599833 IC50 > 1000.0 nM -
CHEMBL599014 IC50 > 1000.0 nM -
CHEMBL3918918 IC50 > 1000.0 nM -