Target Information
| Target General Information | Top | |||||
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| Target ID |
T55948
(Former ID: TTDI01533)
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| Target Name |
Organic cation transporter 3 (OCT3)
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| Synonyms |
Solute carrier family 22 member 3; Extraneuronal monoamine transporter; EMTH
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| Gene Name |
SLC22A3
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| Target Type |
Literature-reported target
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| Function |
Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
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| UniProt ID | ||||||
| Sequence |
MPSFDEALQRVGEFGRFQRRVFLLLCLTGVTFAFLFVGVVFLGTQPDHYWCRGPSAAALA
ERCGWSPEEEWNRTAPASRGPEPPERRGRCQRYLLEAANDSASATSALSCADPLAAFPNR SAPLVPCRGGWRYAQAHSTIVSEFDLVCVNAWMLDLTQAILNLGFLTGAFTLGYAADRYG RIVIYLLSCLGVGVTGVVVAFAPNFPVFVIFRFLQGVFGKGTWMTCYVIVTEIVGSKQRR IVGIVIQMFFTLGIIILPGIAYFIPNWQGIQLAITLPSFLFLLYYWVVPESPRWLITRKK GDKALQILRRIAKCNGKYLSSNYSEITVTDEEVSNPSFLDLVRTPQMRKCTLILMFAWFT SAVVYQGLVMRLGIIGGNLYIDFFISGVVELPGALLILLTIERLGRRLPFAASNIVAGVA CLVTAFLPEGIAWLRTTVATLGRLGITMAFEIVYLVNSELYPTTLRNFGVSLCSGLCDFG GIIAPFLLFRLAAVWLELPLIIFGILASICGGLVMLLPETKGIALPETVDDVEKLGSPHS CKCGRNKKTPVSRSHL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T83ENN | |||||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: (11-BETA)-11,21-DIHYDROXY-PREGN-4-ENE-3,20-DIONE | Ligand Info | |||||
| Structure Description | Structure of human OCT3 in complex with inhibitor Corticosterone | PDB:7ZH6 | ||||
| Method | Electron microscopy | Resolution | 3.67 Å | Mutation | No | [2] |
| PDB Sequence |
SFDEALQRVG
12 EFGRFQRRVF22 LLLCLTGVTF32 AFLFVGVVFL42 GTQPDHYWCR52 GPSAAALAER 62 CGWSPEEEWN72 RTAPASRGRC90 QRYLLSAPLV125 PCRGGWRYAQ135 AHSTIVSEFD 145 LVCVNAWMLD155 LTQAILNLGF165 LTGAFTLGYA175 ADRYGRIVIY185 LLSCLGVGVT 195 GVVVAFAPNF205 PVFVIFRFLQ215 GVFGKGTWMT225 CYVIVTEIVG235 SKQRRIVGIV 245 IQMFFTLGII255 ILPGIAYFIP265 NWQGIQLAIT275 LPSFLFLLYY285 WVVPESPRWL 295 ITRKKGDKAL305 QILRRIAKCN315 VSNPSFLDLV342 RTPQMRKCTL352 ILMFAWFTSA 362 VVYQGLVMRL372 GNLYIDFFIS386 GVVELPGALL396 ILLTIERLGR406 RLPFAASNIV 416 AGVACLVTAF426 LPEGIAWLRT436 TVATLGRLGI446 TMAFEIVYLV456 NSELYPTTLR 466 NFGVSLCSGL476 CDFGGIIAPF486 LLFRLAAVWL496 ELPLIIFGIL506 ASICGGLVML 516 LPETKGIALP526 ETVDDVEK
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| Ligand Name: 1-Ethyl-2-[(1-ethylquinolin-2-yl)methyl]quinoline | Ligand Info | |||||
| Structure Description | Structure of human OCT3 in complex with inhibitor decynium-22 | PDB:7ZHA | ||||
| Method | Electron microscopy | Resolution | 3.55 Å | Mutation | No | [2] |
| PDB Sequence |
SFDEALQRVG
12 EFGRFQRRVF22 LLLCLTGVTF32 AFLFVGVVFL42 GTQPDHYWCR52 GPSAAALAER 62 CGWSPEEEWN72 RTAPASRGRC90 QRYLLEAPLV125 PCRGGWRYAQ135 AHSTIVSEFD 145 LVCVNAWMLD155 LTQAILNLGF165 LTGAFTLGYA175 ADRYGRIVIY185 LLSCLGVGVT 195 GVVVAFAPNF205 PVFVIFRFLQ215 GVFGKGTWMT225 CYVIVTEIVG235 SKQRRIVGIV 245 IQMFFTLGII255 ILPGIAYFIP265 NWQGIQLAIT275 LPSFLFLLYY285 WVVPESPRWL 295 ITRKKGDKAL305 QILRRIAKCN315 GDEEVSNPSF338 LDLVRTPQMR348 KCTLILMFAW 358 FTSAVVYQGL368 VMRLGIIGGN378 LYIDFFISGV388 VELPGALLIL398 LTIERLGRRL 408 PFAASNIVAG418 VACLVTAFLP428 EGIAWLRTTV438 ATLGRLGITM448 AFEIVYLVNS 458 ELYPTTLRNF468 GVSLCSGLCD478 FGGIIAPFLL488 FRLAAVWLEL498 PLIIFGILAS 508 ICGGLVMLLP518 ETKGIALPET528 VDDVEKL
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Similarity Proteins
Human Tissue Distribution
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| Chemical Structure based Activity Landscape of Target | Top |
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| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| References | Top | |||||
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| REF 1 | Electrophysiological Characterization of Novel Effects of the Uptake-2 Blocker Decynium-22 (D-22) on Dopaminergic Neurons in the Substantia Nigra P... Neuroscience. 2019 Jan 1;396:154-165. | |||||
| REF 2 | Structural basis of organic cation transporter-3 inhibition. Nat Commun. 2022 Nov 7;13(1):6714. | |||||
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