BDBM36609 Rapamycin C-7, analog 4::SIROLIMUS::US11603377, Compound Ramycin

SMILES CO[C@@H]1C[C@H](C[C@@H](C)[C@@H]2CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)\[C@H](C[C@@H]3CC[C@@H](C)[C@@](O)(O3)C(=O)C(=O)N3CCCC[C@H]3C(=O)O2)OC)CC[C@H]1O

InChI Key InChIKey=QFJCIRLUMZQUOT-UHFFFAOYSA-N

Data  4 KI  25 IC50  13 Kd  6 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 47 hits for monomerid = 36609   

TargetTarget of rapamycin complex subunit LST8(Human)
Revolution Medicines

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 1.00E+3nMAssay Description:Inhibition of mTORC1 in human MDA-MB-468 cells assessed as reduction in 4EBP1 phosphorylation at Thr37/46 by AlphaLISA assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/13/2024
Entry Details
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of mTOR (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2022
Entry Details Article
PubMed
TargetTarget of rapamycin complex subunit LST8(Human)
Revolution Medicines

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 450nMAssay Description:Inhibition of mTORC1 in human A549 cells assessed as measuring phosphorylated S6K1 level incubated for 2 hrs by Western blot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/26/2023
Entry Details
PubMed
TargetTarget of rapamycin complex subunit LST8(Human)
Revolution Medicines

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 0.0500nMAssay Description:Inhibition of mTORC1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/26/2023
Entry Details
PubMed
TargetBroad substrate specificity ATP-binding cassette transporter ABCG2(Human)
Federal University of Parana

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 1.90E+3nMAssay Description:Inhibition of ABCG2 (unknown origin) expressed in human HEK293 cells mediated pheophorbide A efflux and measured after 90 mins by FACSflow cytometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Aeovian Pharmaceuticals

US Patent
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 Depth
Date in BDB:
4/30/2023
Entry Details
Go to US Patent

TargetPeptidyl-prolyl cis-trans isomerase FKBP5(Human)
Aeovian Pharmaceuticals

US Patent
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKd: <10nMAssay Description:Biotinylated avi-FKBP51 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 Depth
Date in BDB:
4/30/2023
Entry Details
Go to US Patent

TargetPyruvate kinase PKM(Human)
National Institute of Pharmaceutical Education and Research Ahmedabad

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 50nMAssay Description:Inhibition of PKM2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details Article
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP5(Human)
Aeovian Pharmaceuticals

US Patent
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKd:  3.70nMAssay Description:Binding affinity to FKBP51 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKd:  4.20nMAssay Description:Binding affinity to FKBP52 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/22/2024
Entry Details
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 0.100nMAssay Description:Inhibition of human mTORMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetTarget of rapamycin complex subunit LST8(Human)
Revolution Medicines

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 0.0600nMAssay Description:Inhibition of mTORC1 in human MDA-MB-468 cells assessed as reduction in P70S6K phosphorylation at Thr389 by AlphaLISA assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/13/2024
Entry Details
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Aeovian Pharmaceuticals

US Patent
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 Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Revolution Medicines

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataEC50: <10nMAssay Description:Inhibition of recombinant human EmGFP fused FKBP12/GST-tagged human mTOR (1360 to 2549 residues) FRB domain incubated for 1 hrs by LanthaScreen based...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/13/2024
Entry Details
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Aeovian Pharmaceuticals

US Patent
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKd:  0.200nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Aeovian Pharmaceuticals

US Patent
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKd:  12nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 0.0500nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPyruvate kinase PKM(Human)
National Institute of Pharmaceutical Education and Research Ahmedabad

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 50nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 0.100nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Aeovian Pharmaceuticals

US Patent
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKd:  0.130nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1B(Human)
Technical University Darmstadt

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKd:  0.600nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP5(Human)
Aeovian Pharmaceuticals

US Patent
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKd:  8.5nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP4(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKd:  12nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Aeovian Pharmaceuticals

US Patent
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 Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1B(Human)
Technical University Darmstadt

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKd:  0.200nMAssay Description:Binding affinity to FKBP12 (unknown origin) by NMR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2016
Entry Details Article
PubMed
TargetNuclear receptor subfamily 1 group I member 2(Human)
National Institutes of Health Chemical Genomics Center

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataEC50:  1.00E+4nMAssay Description:Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2016
Entry Details Article
PubMed
TargetNuclear receptor subfamily 1 group I member 2(Human)
National Institutes of Health Chemical Genomics Center

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataEC50:  890nMAssay Description:Competitive binding affinity to human PXR LBD (111 to 434) by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2016
Entry Details Article
PubMed
TargetEukaryotic translation initiation factor 4E(Human)
University of Toronto

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKd:  0.5nMAssay Description:Binding affinity to purified elF4EMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2011
Entry Details Article
PubMed
TargetProgrammed cell death protein 4(Human)
National Cancer Institute-Frederick

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataEC50:  50nMAssay Description:Inhibition of TPA-induced degradation of Pdcd4 (amino acid 39-91) expressed in human HEK293 cells assessed as minimum compound concentration required...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/5/2011
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of mTOR-mediated Akt phosphorylation in human PC3 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/22/2012
Entry Details Article
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Aeovian Pharmaceuticals

US Patent
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 Depth
Date in BDB:
9/30/2012
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 0.450nMAssay Description:Inhibitory concentration against FKBP12 receptorMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2012
Entry Details Article
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Aeovian Pharmaceuticals

US Patent
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 Depth
Date in BDB:
12/4/2012
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 3.5nMAssay Description:The inhibitory activity by using FK506 binding protein 12 SPA binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/22/2013
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 0.100nMAssay Description:Inhibition of mTOR kinase expressed in human HEK293 cells by Western blot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2012
Entry Details Article
PubMed
TargetBile salt export pump(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2019
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKd:  0.600nMAssay Description:Binding affinity to mTOR FKBP12 site (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/19/2020
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 430nMAssay Description:Inhibition of mTOR (unknown origin) incubated for 1 hr by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
TargetSolute carrier organic anion transporter family member 1B1(Human)
Deutsches Krebsforschungszentrum

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 1.10E+3nMAssay Description:TP_TRANSPORTER: inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/29/2020
Entry Details Article
PubMed
TargetATP-dependent translocase ABCB1(Human)
Avmax

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 1.25E+3nMAssay Description:TP_TRANSPORTER: inhibition of Rhodamine 123 transport (basal to apical) (R123: 15 uM) in HCT-8 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/29/2020
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase mTOR(Mouse)
Therachem Research Medilab

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 0.0500nMAssay Description:Inhibition of mTOR in mouse TSC1-/- MEF cells assessed as inhibition of S6 Ser240/244 phosphorylation incubated for 2 hrs by fluorescence based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMed
TargetSarcoplasmic/endoplasmic reticulum calcium ATPase 1(Rabbit)
University of Chemistry and Technology Prague

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 7.70E+4nMAssay Description:Inhibition of rabbit SERCA1a preincubated for 10 mins followed by addition of ATP and measured after 10 mins by colorimetric methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase mTOR(Human)
Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre

Curated by ChEMBL
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataIC50: 0.100nMAssay Description:Inhibition of mTOR in HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Aeovian Pharmaceuticals

US Patent
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 Depth
Date in BDB:
11/9/2012
Entry Details Article
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Aeovian Pharmaceuticals

US Patent
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 Depth
Date in BDB:
4/15/2011
Entry Details Article
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP5(Human)
Aeovian Pharmaceuticals

US Patent
LigandPNGBDBM36609(Rapamycin C-7, analog 4 | SIROLIMUS | US11603377, ...)
Affinity DataKi:  3nMAssay Description:Binding affinity to human FKBP51 by competitive fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetPeptidyl-prolyl cis-trans isomerase FKBP1A(Human)
Aeovian Pharmaceuticals

US Patent
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 Depth
Date in BDB:
6/26/2023
Entry Details
PubMed