BAY-390

BAY-390 : Inhibitor of TRPA1

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe BAY-390 is in the process of SERP review.

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Information

TRPA1

Inhibitor

100 nM

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family - Selectivity against family members was tested, all > 30 fold: hTRPV1 IC50 > 25 µM, hTRPV4 IC50 > 25 µM, hTRPC3 IC50 > 25 µM, hTRPC5 IC50 = 5.6 µM, hTRPC6 IC50 > 25 µM, hKCNK9 (TASK-3) IC50 > 30 µM, hCACNA1H (Cav3.2) IC50 > 25 µM. Selectivity outside target family - Selectivity in Eurofins Lead Profiling Screen, GPCR Profiling Screen and Bayer Kinase Panel was performed. Closest off-targets: SLC6A3 (human) Ki = 0.9 μM, PGR (human) Ki = 4 μM, ESR1 EC50 = 2.1 μM. Two off-targets in the GPCR scan: SLC6A3 Ki = 1377.15 nM, HTR2A Ki = 2576.32 nM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 23 Mar 2022 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 14 Apr 2022 )