D6-3

D6-3 : Covalent Inhibitor of CTSL

Structure

SERP Rating

Probe D6-3 is in the process of SERP review.

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Information

CTSL

Covalent Inhibitor

up to 10 uM

In Vitro Validations

Uniprot ID: P07711

Target Class: Enzyme

Target SubClass: Cysteine protease

Potency: IC50

Potency Value: 0.27 nM

Potency Assay: FRET protease assay

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

Target aliases:

Procathepsin L, CTSL1, CTSL, CATL1_HUMAN, MEP, Maj ...

DOI Reference: 10.1021/acs.jmedchem.4c00656

Uniprot ID: P07711

Target Class: Enzyme

Target SubClass: Cysteine protease

Potency Value: Kinact/Ki 6.83 ± 0.25 × 10*6 S-1 M-1

Potency Assay: Kinetic binding assay

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

Target aliases:

Procathepsin L, CTSL1, CTSL, CATL1_HUMAN, MEP, Maj ...

DOI Reference: 10.1021/acs.jmedchem.4c00656

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): D6-3 inhibitor activity was measured on seven human proteases @ 10 uM. Among them, TMPRSS2, human trypsin (hTrypsin), and human chymotrypsin (hChymotrypsin) are serine proteases, and cathepsin B (CatB), cathepsin V (CatV), cathepsin S (CatS), and caspase 3 are cysteine proteases. D6–3 showed no activities against the three serine proteases or caspase 3.

Probe Selectivity in Vitro:

D6-3 did show inhibition against CatB, CatV, and CatS. Kinact/Ki values of D6–3 for other cathepsins were generally 1 to 3 orders of magnitude lower than those of CatL, indicating that D6–3 exhibits better selectivity for CatL

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SERP ratings and comments

No SERP comments found for D6-3