| ID Source | ID |
|---|---|
| PubMed CID | 445501 |
| CHEMBL ID | 6367 |
| SCHEMBL ID | 4766380 |
| MeSH ID | M0273945 |
| Synonym |
|---|
| GPI , |
| (2s)-[3-pyridyl-1-propyl]-1-[3,3-dimethyl-1,2-dioxopentyl]-2-pyrrolidinecarboxylate |
| gpi-1046 |
| 1F40 |
| DB01951 |
| bdbm23334 |
| 3-(pyridin-3-yl)propyl (2s)-1-(3,3-dimethyl-2-oxopentanoyl)pyrrolidine-2-carboxylate |
| chembl6367 , |
| 3-pyridin-3-ylpropyl (2s)-1-(3,3-dimethyl-2-oxopentanoyl)pyrrolidine-2-carboxylate |
| AKOS015994582 |
| (s)-3-(pyridine-3-yl)propyl 1-(3,3-dimethyl-2-oxopentanoyl)pyrrolidine-2-carboxylate |
| AM84643 |
| l-proline, 1-(3,3-dimethyl-1,2-dioxopentyl)-, 3-(3-pyridinyl)propyl ester |
| 186452-09-5 |
| (s)-3-(pyridin-3-yl)propyl 1-(3,3-dimethyl-2-oxopentanoyl)pyrrolidine-2-carboxylate |
| ES-0040 |
| SCHEMBL4766380 |
| DTXSID00332191 |
| 3-pyridin-3-ylpropyl(2s)-1-(3,3-dimethyl-2-oxo-pentanoyl)pyrrolidine-2-carboxylate |
| 3-(3-pyridyl)-1-propyl (2s)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate |
| 3-pyridin-3-ylpropyl 1-(3,3-dimethyl-2-oxopentanoyl)-l-prolinate |
| HY-124619 |
| Q27093051 |
| CS-0087142 |
| A880654 |
| (s)-3-(pyridin-3-yl)propyl1-(3,3-dimethyl-2-oxopentanoyl)pyrrolidine-2-carboxylate |
| gtpl11483 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Peptidyl-prolyl cis-trans isomerase FKBP1A | Bos taurus (cattle) | Ki | 0.0075 | 0.0075 | 0.0075 | 0.0075 | AID1798315 |
| Serine/threonine-protein kinase mTOR | Homo sapiens (human) | IC50 (µMol) | 20.8930 | 0.0000 | 0.8575 | 10.0000 | AID69259 |
| Peptidyl-prolyl cis-trans isomerase FKBP1A | Homo sapiens (human) | IC50 (µMol) | 1.2400 | 0.0004 | 0.3937 | 3.6000 | AID672586 |
| Peptidyl-prolyl cis-trans isomerase FKBP1A | Homo sapiens (human) | Ki | 0.0050 | 0.0000 | 0.8837 | 5.4000 | AID198616; AID69102; AID69110 |
| Peptidyl-prolyl cis-trans isomerase FKBP4 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0160 | 5.1287 | 8.0000 | AID672588 |
| Peptidyl-prolyl cis-trans isomerase FKBP5 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 8.5200 | 8.5200 | 8.5200 | AID672587 |
| Peptidyl-prolyl cis-trans isomerase FKBP1A | Rattus norvegicus (Norway rat) | Ki | 0.0075 | 0.0075 | 0.0075 | 0.0075 | AID69115 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, FK506 BINDING PROTEIN (FKBP12) | Homo sapiens (human) | Kd | 1.0000 | 1.0000 | 1.0000 | 1.0000 | AID977611 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID123532 | Percent recovery of tyrosine hydroxylase immunostaining after oral administration at dose 10 mg/kg concurrently with MPTP | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects. |
| AID69259 | The inhibitory activity by using FK506 binding protein 12 SPA binding assay | 2000 | Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10 | Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands. |
| AID117556 | Post-MPTP % recovery of striatal dopaminergic innervation relative to MPTP-treated mice after peroral administration at dose of 10 mg/kg | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands. |
| AID672587 | Binding affinity to FKBP51 FK1 domain by fluorescence polarization assay | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52. |
| AID123534 | Percent recovery of tyrosine hydroxylase immunostaining in mice following 10 mg/kg s.c. administration concurrently with MPTP. | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects. |
| AID268882 | Neurotrophic activity in chick dorsal root ganglion at 100 pM in presence of NGF after 48 hrs relative to control | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Modeling and synthesis of non-cyclic derivatives of GPI-1046 as potential FKBP ligands with neurotrophic properties. |
| AID53013 | In vitro promotion of fiber extension (neurite outgrowth) from cultured chick sensory neuron | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects. |
| AID136435 | Recovery of TH-immunostaining in MTTP-treated mice by post-MPTP treatment at a peroral dose of 10 mg/kg | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10 | Solid-phase synthesis of FKBP12 inhibitors: N-sulfonyl and N-carbamoylprolyl/pipecolyl amides. |
| AID672586 | Binding affinity to FKBP12 by fluorescence polarization assay | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52. |
| AID672588 | Binding affinity to FKBP52 FK1 domain by fluorescence polarization assay | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52. |
| AID198616 | The compound was tested for binding affinity against rotamase | 1998 | Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21 | Investigations of neurotrophic inhibitors of FK506 binding protein via Monte Carlo simulations. |
| AID117554 | Concurrent % recovery of striatal dopaminergic innervation relative to MPTP-treated mice after subcutaneous administration at dose of 4 mg/kg. | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands. |
| AID69115 | In vitro inhibition of rotamase activity of FK506 binding protein 12 | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands. |
| AID50628 | The compound was evaluated for neurite outgrowth from chick dorsal root ganglia | 1998 | Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21 | Investigations of neurotrophic inhibitors of FK506 binding protein via Monte Carlo simulations. |
| AID69102 | Ability to inhibit peptidyl-prolyl isomerase (PPIase, or rotamase) activity of FK506 binding protein 12 | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10 | Solid-phase synthesis of FKBP12 inhibitors: N-sulfonyl and N-carbamoylprolyl/pipecolyl amides. |
| AID123533 | Percent recovery of tyrosine hydroxylase immunostaining after peroral administration at dose 10 mg/kg after lesioning with MPTP (post-MPTP) | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects. |
| AID69110 | Inhibitory activity against FK506 binding protein 12 | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects. |
| AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2000 | European journal of biochemistry, Sep, Volume: 267, Issue:17 | Solution structure of a neurotrophic ligand bound to FKBP12 and its effects on protein dynamics. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2000 | European journal of biochemistry, Sep, Volume: 267, Issue:17 | Solution structure of a neurotrophic ligand bound to FKBP12 and its effects on protein dynamics. |
| AID1798315 | Peptidyl Prolyl Isomerase (PPIase) Inibition Assay from Article 10.1021/jm0200456: \\Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands.\\ | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (12.50) | 18.2507 |
| 2000's | 6 (75.00) | 29.6817 |
| 2010's | 1 (12.50) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (12.17) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 8 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||