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Report error Found 9 Enz. Inhib. hit(s) for PDB: 2DG9
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Guilford Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKi:  0.200nMAssay Description:Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activityMore data for this Ligand-Target Pair
In DepthDetails
ArticlePubMedPDB3D3D Structure (crystal)
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Guilford Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKi:  1nM EC50:  30nMAssay Description:FKBP12 assay using rapamycin analogs.More data for this Ligand-Target Pair
In DepthDetails
ArticlePubMedPDB3D3D Structure (crystal)
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Guilford Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKi:  5.40E+3nMAssay Description:Binding affinity to FKBP12 (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In DepthDetails
PubMedPDB3D3D Structure (crystal)
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Guilford Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50:  0.450nMAssay Description:Inhibitory concentration against binding to FKBP12More data for this Ligand-Target Pair
In DepthDetails
ArticlePubMedPDB3D3D Structure (crystal)
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Guilford Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50:  0.600nMAssay Description:Compound was tested in vitro for its ability to compete with immobilized FK506 for binding to biotinylated FK506 binding protein 12 in a competitive ...More data for this Ligand-Target Pair
In DepthDetails
ArticlePubMedPDB3D3D Structure (crystal)
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Guilford Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50064359(1,18-Dihydroxy-12-[2-(4-hydroxy-3-methoxy-cyclohex...)
Affinity DataIC50:  1.10nMAssay Description:Inhibitory binding activity against human Immunophilin-FK506 binding protein 12More data for this Ligand-Target Pair
In DepthDetails
ArticlePubMedPDB3D3D Structure (crystal)
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Guilford Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50:  20nMAssay Description:Displacement of fluorescent tracer Rap-Gly-BDP from nanoluciferse-tagged human FKBP12 expressed in HEK293T cells incubated for 2 hrs by NanoBRET assa...More data for this Ligand-Target Pair
In DepthDetails
ArticlePubMedPDB3D3D Structure (crystal)
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Guilford Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataEC50:  36nMAssay Description:Binding affinity to FKBP12 (unknown origin) expressed in HEK293 cells co-expressing FRB assessed as induction of FKBP12-FRB dimerization measured for...More data for this Ligand-Target Pair
In DepthDetails
ArticlePubMedPDB3D3D Structure (crystal)
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Guilford Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKd: <0.300nMAssay Description:Biotinylated avi-FKBP12 was immobilized on a streptavidin chip (Cytiva Series S SA) using a Biacore 8K or 8 k+ (Cytiva). To achieve an immobilization...More data for this Ligand-Target Pair
In DepthDetails
US Patent
PDB3D3D Structure (crystal)