Tacrolimus

Tacrolimus : Inhibitor, Molecular Glue of FKBP1A

Structure

SERP Rating

In Cells

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In Model Organisms

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Information

FKBP1A

Molecular Glue

up to 1 uM

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Probe Availability:

In Vitro Validations

Uniprot ID: P62942

Target Class: Other

Target SubClass: Immunophilin Protein Family

Potency: Kd

Potency Value: 0.4 nM

Potency Assay: Spectrophotometric Assay (Fisher Assay)

PDB ID for probe-target interaction (3D structure): 1FKF

Structure-activity relationship: No

Target aliases:

Peptidyl-prolyl cis-trans isomerase FKBP1A, FKBP12 ...

DOI Reference: 10.1073/pnas.89.9.3686

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency end-point : Ki FKBP12.6 0.55 nM, FKBP37 4 nM, FKBP52 10 nM, CyP-A 2 nM, CyP-C 4 nM, CyP-D 3.6 nM

Probe Selectivity in Vitro:

Activity (Ki) against FKBP human immunophilins: FKBP12.6 0.55 nM, FKBP13 38 nM, FKBP25 160 nM, FKBP37 4 nM and FKBP52 10 nM. Activity (Ki) against human Cyclophilins CyP-A 2 nM, CyP-B 84 nM, CyP-C 4 nM, CyP-D 3.6 nM, CyP-40 300 nM, and CyP-NK N/A.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 4 Jan 2022 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 11 Jan 2022 )