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

CHEMBL3424026

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

Binding
Antagonist activity against rat TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced intracellular Ca2+ level pre-treated 5 mins before icilin stimulation by Fluo-4-AM dye based spectrofluorimetry
ChEMBL ↗
54
Total Activities
54
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

Transient receptor potential cation channel subfamily M member 8 (CHEMBL5011) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationships of the prototypical TRPM8 agonist icilin.
De Petrocellis L, Ortar G, Schiano Moriello A, Serum EM, Rusterholz DB.
Bioorg Med Chem Lett (2015) 25 : 2285 -2290
PubMed 25935641 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 5.53 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL258405 ICILLIN 3.0 1 7.24
CHEMBL3422837 — — 1 7.14
CHEMBL3422836 — — 1 6.85
CHEMBL3422842 — — 1 6.77
CHEMBL3422835 — — 1 6.77
CHEMBL3422796 — — 1 6.62
CHEMBL3422799 — — 1 6.58
CHEMBL3422840 — — 1 6.40
CHEMBL3422838 — — 1 6.37
CHEMBL3422811 — — 1 6.33
CHEMBL3422843 — — 1 6.22
CHEMBL3422806 — — 1 6.02
CHEMBL3422807 — — 1 5.99
CHEMBL3422834 — — 1 5.98
CHEMBL3422830 — — 1 5.96
CHEMBL3422798 — — 1 5.85
CHEMBL3422794 — — 1 5.82
CHEMBL3422833 — — 1 5.82
CHEMBL3422810 — — 1 5.82
CHEMBL2251560 — — 1 5.77
CHEMBL3422829 — — 1 5.75
CHEMBL3422827 — — 1 5.72
CHEMBL3422839 — — 1 5.70
CHEMBL3422826 — — 1 5.51
CHEMBL3422808 — — 1 5.50
CHEMBL3422820 — — 1 5.46
CHEMBL3422809 — — 1 5.36
CHEMBL3422823 — — 1 5.24
CHEMBL3422814 — — 1 5.24
CHEMBL3422841 — — 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL258405 ICILLIN IC50 = 58.0 nM 7.24
CHEMBL3422837 — IC50 = 73.0 nM 7.14
CHEMBL3422836 — IC50 = 140.0 nM 6.85
CHEMBL3422842 — IC50 = 170.0 nM 6.77
CHEMBL3422835 — IC50 = 170.0 nM 6.77
CHEMBL3422796 — IC50 = 240.0 nM 6.62
CHEMBL3422799 — IC50 = 260.0 nM 6.58
CHEMBL3422840 — IC50 = 400.0 nM 6.40
CHEMBL3422838 — IC50 = 430.0 nM 6.37
CHEMBL3422811 — IC50 = 470.0 nM 6.33
CHEMBL3422843 — IC50 = 600.0 nM 6.22
CHEMBL3422806 — IC50 = 950.0 nM 6.02
CHEMBL3422807 — IC50 = 1030.0 nM 5.99
CHEMBL3422834 — IC50 = 1050.0 nM 5.98
CHEMBL3422830 — IC50 = 1100.0 nM 5.96
CHEMBL3422798 — IC50 = 1400.0 nM 5.85
CHEMBL3422794 — IC50 = 1500.0 nM 5.82
CHEMBL3422833 — IC50 = 1500.0 nM 5.82
CHEMBL3422810 — IC50 = 1500.0 nM 5.82
CHEMBL2251560 — IC50 = 1700.0 nM 5.77
CHEMBL3422829 — IC50 = 1800.0 nM 5.75
CHEMBL3422827 — IC50 = 1900.0 nM 5.72
CHEMBL3422839 — IC50 = 2000.0 nM 5.70
CHEMBL3422826 — IC50 = 3100.0 nM 5.51
CHEMBL3422808 — IC50 = 3200.0 nM 5.50
CHEMBL3422820 — IC50 = 3500.0 nM 5.46
CHEMBL3422809 — IC50 = 4400.0 nM 5.36
CHEMBL3422823 — IC50 = 5700.0 nM 5.24
CHEMBL3422814 — IC50 = 5700.0 nM 5.24
CHEMBL3422841 — IC50 = 6100.0 nM 5.21
CHEMBL3422832 — IC50 = 6500.0 nM 5.19
CHEMBL3422824 — IC50 = 6600.0 nM 5.18
CHEMBL1451030 — IC50 = 8300.0 nM 5.08
CHEMBL3422802 — IC50 = 8300.0 nM 5.08
CHEMBL3422805 — IC50 = 8700.0 nM 5.06
CHEMBL3422815 — IC50 = 10900.0 nM 4.96
CHEMBL3422795 — IC50 = 11300.0 nM 4.95
CHEMBL3422817 — IC50 = 11400.0 nM 4.94
CHEMBL3422816 — IC50 = 11400.0 nM 4.94
CHEMBL3422819 — IC50 = 11400.0 nM 4.94
CHEMBL3422800 — IC50 = 12000.0 nM 4.92
CHEMBL3422812 — IC50 = 14300.0 nM 4.84
CHEMBL3422801 — IC50 = 15700.0 nM 4.80
CHEMBL3422818 — IC50 = 16900.0 nM 4.77
CHEMBL3422825 — IC50 = 18100.0 nM 4.74
CHEMBL3422803 — IC50 = 22000.0 nM 4.66
CHEMBL3422822 — IC50 = 26000.0 nM 4.58
CHEMBL3422821 — IC50 = 33900.0 nM 4.47
CHEMBL3422797 — IC50 = 40000.0 nM 4.40
CHEMBL3422804 — IC50 = 46400.0 nM 4.33