TTBK1-IN-1

Details for TTBK1-IN-1 : Inhibitor of TTBK1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe TTBK1-IN-1 is in the process of SERP review.

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Information

TTBK1
TTBK2

Inhibitor

up to 1 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: Q5TCY1

Target Class: Kinase

Target SubClass: CK1

Potency: IC50

Potency Value: 2.7 nM

Potency Assay: Biochemical assay (TR-FRET assay)

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

Target aliases:

Tau-tubulin kinase 1, KIAA1855, BDTK, TTBK1, TTBK1 ...

DOI Reference: 10.1021/acs.jmedchem.1c00382

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): KinomeSCAN (DiscoverX kinome panel (468 kinases)) was performed at 100 and 1000 nM. TTBK1-IN-1 was tested against the major off-target kinases observed in the kinome panel revealing that only CK1δ and PRKD1 were inhibited with less than a 20-fold selectivity over TTBK1 and that TTBK1-IN-1 had very weak activity against NIK (>400-fold selectivity vs TTBK1). Outside target family: TTBK1-IN-1 was also evaluated in a Eurofins panel against 68 common target proteins which revealed that only Adenosine A1, A2A, and A3 were potential off targets (61, 64, and 73% inhibition, respectively, at a 10 μM test concentration).

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

As the PK data is incomplete, the in vivo rating is only 3 stars.

(last updated: 23 Oct 2023 )