HM-279

HM-279 : Inhibitor of TGFBR1

Structure

SERP Rating

Probe HM-279 is in the process of SERP review.

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Information

TGFBR1

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: P36897

Target Class: Kinase

Target SubClass: TKL

Potency: IC50

Potency Value: 4.7 nM

Potency Assay: Biochemical assay

PDB ID for probe-target interaction (3D structure): 9J9D

Target aliases:

TGF-beta receptor type-1, TGFBR1, TGFR1_HUMAN, Tbe ...

DOI Reference: 10.1021/acs.jmedchem.4c02293

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Off Target: ACVR1C

Potency end-point : IC50 6.8 nM

Potency assay (off target): HM-279 was evaluated in a panel of 10 TGF-β receptor family kinases. HM-279 showed cross-reactivity with ALK7 (IC50 = 6.8 nM), but has fair to good selectivity against other TGF-β receptor family members, with 4.5–693-fold selectivity. 16 fold selectivity over TrkC and 24 fold selectivity over AurC kinases.

Potency assay (off target): Kinome-wide selectivity of HM-279 was also assessed in a panel of 255 kinase assays. HM-279 exhibited an excellent kinase selectivity and inhibited only 9 kinases: AurA, BUB1/BUB3, FLT4, KDR, NuaK1, PDGFRα, PDGFRβ, QIK, and MST1 (>70% inhibition at 0.1 μM).

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