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Assay Detail

CHEMBL1954858

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

Functional
Antagonist activity at rat TRPA1 ion channel expressed in HEK293 cells assessed as inhibition of AITC-induced calcium influx incubated for 5 mins prior to AITC-induction by fluo-4-AM-based fluorimetry
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Synthesis and biological evaluation of [6]-gingerol analogues as transient receptor potential channel TRPV1 and TRPA1 modulators.
Morera E, De Petrocellis L, Morera L, Moriello AS, Nalli M, Di Marzo V, Ortar G.
Bioorg Med Chem Lett (2012) 22 : 1674 -1677
PubMed 22257892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 4.94 5.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1950598 1 5.64
CHEMBL1950584 1 5.55
CHEMBL1950593 1 5.55
CHEMBL1950590 1 5.48
CHEMBL1950595 1 5.44
CHEMBL1950587 1 5.41
CHEMBL487732 1 5.35
CHEMBL1950594 1 4.96
CHEMBL1950597 1 4.84
CHEMBL1950589 1 4.84
CHEMBL1950596 1 4.80
CHEMBL25948 SHOGAOL 1 4.78
CHEMBL1950586 1 4.65
CHEMBL1097449 1 4.46
CHEMBL1950592 1 4.42
CHEMBL1950591 1 4.40
CHEMBL1950585 1 4.25
CHEMBL1950588 1 4.01
CHEMBL1950582 1 -
CHEMBL1950583 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1950598 IC50 = 2300.0 nM 5.64
CHEMBL1950584 IC50 = 2800.0 nM 5.55
CHEMBL1950593 IC50 = 2800.0 nM 5.55
CHEMBL1950590 IC50 = 3300.0 nM 5.48
CHEMBL1950595 IC50 = 3600.0 nM 5.44
CHEMBL1950587 IC50 = 3900.0 nM 5.41
CHEMBL487732 IC50 = 4500.0 nM 5.35
CHEMBL1950594 IC50 = 11100.0 nM 4.96
CHEMBL1950597 IC50 = 14300.0 nM 4.84
CHEMBL1950589 IC50 = 14400.0 nM 4.84
CHEMBL1950596 IC50 = 15800.0 nM 4.80
CHEMBL25948 SHOGAOL IC50 = 16700.0 nM 4.78
CHEMBL1950586 IC50 = 22600.0 nM 4.65
CHEMBL1097449 IC50 = 35100.0 nM 4.46
CHEMBL1950592 IC50 = 38200.0 nM 4.42
CHEMBL1950591 IC50 = 39700.0 nM 4.40
CHEMBL1950585 IC50 = 56100.0 nM 4.25
CHEMBL1950588 IC50 = 97850.0 nM 4.01
CHEMBL1950582 IC50 > 100000.0 nM -
CHEMBL1950583 IC50 > 100000.0 nM -