SAFit2

SAFit2 : Antagonist of FKBP5

Structure

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Probe SAFit2 is in the process of SERP review.

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Information

FKBP5

Antagonist

up to 5 µM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: Q13451

Target Class: Enzyme

Target SubClass: Prolyl isomerase

Potency: Kd

Potency Value: 6 ± 2 nM

Potency Assay: competitive fluorescence polarization (FP) assay

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

Target aliases:

Peptidyl-prolyl cis-trans isomerase FKBP5, FKBP51, ...

DOI Reference: 10.1021/acs.jmedchem.5b01355

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: Competitive fluorescence polarization assay: FKBP1B (Kd = 38.9 ± 3.0 nM); FKBP1A (Kd = 116.4 ± 7.1 nM); FKBP2 (Kd = 1053 ± 93 nM); FKBP4 (Kd > 50 μM); FKBP3 (Kd > 10 μM). Selectivity outside target family: GPCR scan (PDSP) 45 targets at 10 μM: Off-targets are TMEM97 (Ki =226 nM) and HRH4 (Ki = 3.5 μM).

Potency assay, off target (cells): NanoBRET assay (HEK293T cell line FKBP51-NLuc): FKBP1A (IC50 = 1103 ± 86 nM)

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