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Assay Detail

CHEMBL4347276

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Binding
Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy
ChEMBL ↗
46
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Transient receptor potential cation channel subfamily A member 1 (CHEMBL6007) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites.
Chandrabalan A, McPhillie MJ, Morice AH, Boa AN, Sadofsky LR.
Eur J Med Chem (2019) 170 : 141 -156
PubMed 30878828 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 5.03 7.10
pIC50 10 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3697701 A-079 — 2 7.10
CHEMBL4456015 — — 2 5.40
CHEMBL593902 AP18 5 — 2 5.40
CHEMBL4454519 — — 2 5.05
CHEMBL4454627 — — 2 5.00
CHEMBL4517528 — — 2 5.00
CHEMBL1079664 — — 2 4.92
CHEMBL1086310 — — 2 4.75
CHEMBL4562546 — — 2 4.60
CHEMBL4516367 — — 2 4.40
CHEMBL4446136 — — 2 4.30
CHEMBL4551396 — — 2 4.00
CHEMBL1081755 — — 2 -
CHEMBL492219 — — 2 -
CHEMBL4515858 — — 2 -
CHEMBL4586540 — — 2 -
CHEMBL242002 — — 2 -
CHEMBL4458679 — — 2 -
CHEMBL4460424 — — 2 -
CHEMBL415324 TRANILAST 3.0 2 -
CHEMBL4557362 — — 2 -
CHEMBL4446849 — — 2 -
CHEMBL4461696 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3697701 A-079 IC50 = 79.43 nM 7.10
CHEMBL3697701 A-079 IC50 = 79.0 nM 7.10
CHEMBL593902 AP18 5 IC50 = 4000.0 nM 5.40
CHEMBL4456015 — IC50 = 4000.0 nM 5.40
CHEMBL4456015 — IC50 = 3981.07 nM 5.40
CHEMBL593902 AP18 5 IC50 = 4466.84 nM 5.35
CHEMBL4454519 — IC50 = 9000.0 nM 5.05
CHEMBL4454519 — IC50 = 10000.0 nM 5.00
CHEMBL4517528 — IC50 = 10000.0 nM 5.00
CHEMBL4454627 — IC50 = 10000.0 nM 5.00
CHEMBL4454627 — IC50 = 10000.0 nM 5.00
CHEMBL4517528 — IC50 = 11000.0 nM 4.96
CHEMBL1079664 — IC50 = 12000.0 nM 4.92
CHEMBL1079664 — IC50 = 12589.25 nM 4.90
CHEMBL1086310 — IC50 = 18000.0 nM 4.75
CHEMBL1086310 — IC50 = 17782.79 nM 4.75
CHEMBL4562546 — IC50 = 25118.86 nM 4.60
CHEMBL4562546 — IC50 = 26000.0 nM 4.58
CHEMBL4516367 — IC50 = 39810.72 nM 4.40
CHEMBL4516367 — IC50 = 43000.0 nM 4.37
CHEMBL4446136 — IC50 = 50118.72 nM 4.30
CHEMBL4446136 — IC50 = 51000.0 nM 4.29
CHEMBL4551396 — IC50 = 100000.0 nM 4.00
CHEMBL4461696 — pIC50 - — -
CHEMBL4446849 — pIC50 - — -
CHEMBL4557362 — pIC50 - — -
CHEMBL415324 TRANILAST IC50 = 125892.54 nM -
CHEMBL492219 — pIC50 - — -
CHEMBL4515858 — pIC50 - — -
CHEMBL4586540 — pIC50 - — -
CHEMBL242002 — pIC50 - — -
CHEMBL4458679 — pIC50 - — -
CHEMBL4460424 — pIC50 - — -
CHEMBL1081755 — IC50 - — -
CHEMBL4461696 — IC50 - — -
CHEMBL4446849 — IC50 - — -
CHEMBL1081755 — pIC50 - — -
CHEMBL4458679 — IC50 - — -
CHEMBL242002 — IC50 - — -
CHEMBL4586540 — IC50 - — -
CHEMBL4515858 — IC50 - — -
CHEMBL492219 — IC50 - — -
CHEMBL4460424 — IC50 - — -
CHEMBL415324 TRANILAST IC50 = 126000.0 nM -
CHEMBL4551396 — IC50 = 106000.0 nM -
CHEMBL4557362 — IC50 - — -