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Assay Detail

CHEMBL1820156

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Functional
Agonist activity at rat TRPA1 channel expressed in HEK293 cells assessed as calcium influx measured at every 1 second for 60 seconds by fluorescence analysis
10
Total Activities
10
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

Design and pharmacological evaluation of PF-4840154, a non-electrophilic reference agonist of the TrpA1 channel.
Ryckmans T, Aubdool AA, Aubdool AA, Bodkin JV, Cox P, Brain SD, Dupont T, Fairman E, Hashizume Y, Ishii N, Kato T, Kitching L, Newman J, Omoto K, Rawson D, Strover J.
Bioorg Med Chem Lett (2011) 21 : 4857 -4859
PubMed 21741838 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 6.20 7.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1818218 1 7.01
CHEMBL1818209 1 6.76
CHEMBL1818214 1 6.73
CHEMBL1818210 1 6.67
CHEMBL1818215 1 6.33
CHEMBL1818212 1 6.24
CHEMBL1818217 1 6.07
CHEMBL1818211 1 5.65
CHEMBL1818213 1 5.25
CHEMBL233248 ALLYL ISOTHIOCYANATE 1.0 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1818218 EC50 = 97.0 nM 7.01
CHEMBL1818209 EC50 = 175.0 nM 6.76
CHEMBL1818214 EC50 = 186.0 nM 6.73
CHEMBL1818210 EC50 = 215.0 nM 6.67
CHEMBL1818215 EC50 = 468.0 nM 6.33
CHEMBL1818212 EC50 = 581.0 nM 6.24
CHEMBL1818217 EC50 = 848.0 nM 6.07
CHEMBL1818211 EC50 = 2250.0 nM 5.65
CHEMBL1818213 EC50 = 5600.0 nM 5.25
CHEMBL233248 ALLYL ISOTHIOCYANATE EC50 = 5813.0 nM 5.24