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Assay Detail

CHEMBL891342

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

Binding
Inhibition of calcium channel L type in IMR32 cells
41
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type IMR-32
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers.
Knutsen LJ, Hobbs CJ, Earnshaw CG, Fiumana A, Gilbert J, Mellor SL, Radford F, Smith NJ, Birch PJ, Russell Burley J, Ward SD, James IF.
Bioorg Med Chem Lett (2007) 17 : 662 -667
PubMed 17134896 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 5.15 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL30008 FLUNARIZINE 2.0 1 6.11
CHEMBL29188 LOMERIZINE 2.0 1 5.83
CHEMBL412849 1 5.70
CHEMBL234510 1 5.68
CHEMBL245171 1 5.66
CHEMBL231820 1 5.63
CHEMBL390705 1 5.54
CHEMBL389993 1 5.51
CHEMBL234915 1 5.38
CHEMBL232848 1 5.37
CHEMBL234916 1 5.37
CHEMBL234490 1 5.34
CHEMBL395982 1 5.33
CHEMBL243019 1 5.26
CHEMBL268157 1 5.26
CHEMBL231799 1 5.21
CHEMBL395109 1 5.18
CHEMBL234943 1 5.13
CHEMBL234914 1 5.09
CHEMBL245173 1 5.09
CHEMBL234938 1 5.08
CHEMBL390703 1 5.02
CHEMBL233855 1 5.00
CHEMBL389103 1 4.99
CHEMBL232032 1 4.99
CHEMBL390704 1 4.94
CHEMBL234491 1 4.93
CHEMBL398157 1 4.90
CHEMBL232849 2 4.89
CHEMBL394578 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL30008 FLUNARIZINE IC50 = 780.0 nM 6.11
CHEMBL29188 LOMERIZINE IC50 = 1480.0 nM 5.83
CHEMBL412849 IC50 = 2010.0 nM 5.70
CHEMBL234510 IC50 = 2080.0 nM 5.68
CHEMBL245171 IC50 = 2180.0 nM 5.66
CHEMBL231820 IC50 = 2330.0 nM 5.63
CHEMBL390705 IC50 = 2920.0 nM 5.54
CHEMBL389993 IC50 = 3080.0 nM 5.51
CHEMBL234915 IC50 = 4160.0 nM 5.38
CHEMBL234916 IC50 = 4250.0 nM 5.37
CHEMBL232848 IC50 = 4230.0 nM 5.37
CHEMBL234490 IC50 = 4580.0 nM 5.34
CHEMBL395982 IC50 = 4690.0 nM 5.33
CHEMBL268157 IC50 = 5440.0 nM 5.26
CHEMBL243019 IC50 = 5540.0 nM 5.26
CHEMBL231799 IC50 = 6200.0 nM 5.21
CHEMBL395109 IC50 = 6660.0 nM 5.18
CHEMBL234943 IC50 = 7490.0 nM 5.13
CHEMBL234914 IC50 = 8030.0 nM 5.09
CHEMBL245173 IC50 = 8200.0 nM 5.09
CHEMBL234938 IC50 = 8410.0 nM 5.08
CHEMBL390703 IC50 = 9510.0 nM 5.02
CHEMBL233855 IC50 = 9990.0 nM 5.00
CHEMBL389103 IC50 = 10300.0 nM 4.99
CHEMBL232032 IC50 = 10300.0 nM 4.99
CHEMBL390704 IC50 = 11500.0 nM 4.94
CHEMBL234491 IC50 = 11700.0 nM 4.93
CHEMBL398157 IC50 = 12500.0 nM 4.90
CHEMBL398158 IC50 = 12900.0 nM 4.89
CHEMBL232849 IC50 = 12900.0 nM 4.89
CHEMBL394578 IC50 = 12900.0 nM 4.89
CHEMBL234698 IC50 = 13700.0 nM 4.86
CHEMBL234273 IC50 = 15000.0 nM 4.82
CHEMBL232034 IC50 = 16400.0 nM 4.79
CHEMBL390187 IC50 = 18200.0 nM 4.74
CHEMBL231826 IC50 = 20600.0 nM 4.69
CHEMBL398158 IC50 = 22900.0 nM 4.64
CHEMBL232849 IC50 = 23200.0 nM 4.63
CHEMBL234274 IC50 = 29300.0 nM 4.53
CHEMBL234511 IC50 > 30000.0 nM -
CHEMBL234719 IC50 > 30000.0 nM -