TDI-10229

TDI-10229 : Inhibitor of ADCY10

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe TDI-10229 is in the process of SERP review.

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Information

ADCY10

Inhibitor

up to 1 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: Q96PN6

Target Class: Enzyme

Target SubClass: Adenylyl Cyclase

Potency: IC50

Potency Value: 195 nM

Potency Assay: In-Vitro Cyclase Activity Assay

PDB ID for probe-target interaction (3D structure): 7OVD

Target aliases:

Adenylate cyclase type 10, SAC, ADCY10, ADCYA_HUMA ...

DOI Reference: 10.1021/acsmedchemlett.1c00273

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): TDI-10229 did not show appreciable activity against a panel of 310 kinases and 46 other well-known drug targets (GPCRs, ion channels, and nuclear receptors). TDI-10229 also displayed high selectivity for sAC versus the closely related tmAC subtypes.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

TDI-10229 appears to be a potent sAC inhibitor that is active both in vitro against purified enzyme and in cell assays of cAMP accumulation. Limited pharmacokinetic data provided for ip and po dosing in mice suggests that TDI-10229 has good exposure, however, data supporting a claim of 59% oral bioavailability in mouse were not provided. No data are provided on microsomal clearance in any model species. TDI-10229 is further claimed to be selective for sAC based on the lack of significant activity against a panel of 310 kinases and 46 other well-known drug targets (GPCRs, ion channels, and nuclear receptors), but again no data to support this claim have been provided.

(last updated: 29 Aug 2023 )