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Assay Detail

CHEMBL1118249

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Functional
Agonist activity at mouse TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium influx
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents.
Baraldi PG, Preti D, Materazzi S, Geppetti P.
J Med Chem (2010) 53 : 5085 -5107
PubMed 20356305 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 5.40 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL193 NIFEDIPINE 4.0 1 6.40
CHEMBL1484 NICARDIPINE 4.0 1 6.30
CHEMBL1428 NIMODIPINE 4.0 1 6.10
CHEMBL475534 NITRENDIPINE 3.0 1 5.42
CHEMBL105672 1 4.68
CHEMBL1082832 1 4.49
CHEMBL283013 1 4.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL193 NIFEDIPINE EC50 = 400.0 nM 6.40
CHEMBL1484 NICARDIPINE EC50 = 500.0 nM 6.30
CHEMBL1428 NIMODIPINE EC50 = 800.0 nM 6.10
CHEMBL475534 NITRENDIPINE EC50 = 3800.0 nM 5.42
CHEMBL105672 EC50 = 20800.0 nM 4.68
CHEMBL1082832 EC50 = 32700.0 nM 4.49
CHEMBL283013 EC50 = 41500.0 nM 4.38