Target Information
| Target General Information | Top | |||||
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| Target ID |
T74166
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| Target Name |
Neuronal acetylcholine receptor alpha-3/beta-4 (CHRNA3/B4)
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| Synonyms |
Neuronal acetylcholine receptor
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| Gene Name |
CHRNA3-CHRNB4
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Cough [ICD-11: MD12] | |||||
| Function |
A type of nicotinic acetylcholine receptor, consisting of 3 and 4 subunits.
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| BioChemical Class |
Neurotransmitter receptor
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| UniProt ID | ||||||
| Sequence |
MRRAPSLVLFFLVALCGRGNCRVANAEEKLMDDLLNKTRYNNLIRPATSSSQLISIKLQL
SLAQLISVNEREQIMTTNVWLKQEWTDYRLTWNSSRYEGVNILRIPAKRIWLPDIVLYNN ADGTYEVSVYTNLIVRSNGSVLWLPPAIYKSACKIEVKYFPFDQQNCTLKFRSWTYDHTE IDMVLMTPTASMDDFTPSGEWDIVALPGRRTVNPQDPSYVDVTYDFIIKRKPLFYTINLI IPCVLTTLLAILVFYLPSDCGEKMTLCISVLLALTFFLLLISKIVPPTSLDVPLIGKYLM FTMVLVTFSIVTSVCVLNVHHRSPSTHTMAPWVKRCFLHKLPTFLFMKRPGPDSSPARAF PPSKSCVTKPEATATSTSPSNFYGNSMYFVNPASAASKSPAGSTPVAIPRDFWLRSSGRF RQDVQEALEGVSFIAQHMKNDDEDQSVVEDWKYVAMVVDRLFLWVFMFVCVLGTVGLFLP PLFQTHAASEGPYAAQRDMGSGPLSLPLALSPPRLLLLLLLSLLPVARASEAEHRLFERL FEDYNEIIRPVANVSDPVIIHFEVSMSQLVKVDEVNQIMETNLWLKQIWNDYKLKWNPSD YGGAEFMRVPAQKIWKPDIVLYNNAVGDFQVDDKTKALLKYTGEVTWIPPAIFKSSCKID VTYFPFDYQNCTMKFGSWSYDKAKIDLVLIGSSMNLKDYWESGEWAIIKAPGYKHDIKYN CCEEIYPDITYSLYIRRLPLFYTINLIIPCLLISFLTVLVFYLPSDCGEKVTLCISVLLS LTVFLLVITETIPSTSLVIPLIGEYLLFTMIFVTLSIVITVFVLNVHYRTPTTHTMPSWV KTVFLNLLPRVMFMTRPTSNEGNAQKPRPLYGAELSNLNCFSRAESKGCKEGYPCQDGMC GYCHHRRIKISNFSANLTRSSSSESVDAVLSLSALSPEIKEAIQSVKYIAENMKAQNEAK EIQDDWKYVAMVIDRIFLWVFTLVCILGTAGLFLQPLMAREDA Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Levopropoxyphene Napsylate Anhydrous | Drug Info | Approved | Cough | [2] | |
| Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
| 1 | TC-5214 | Drug Info | Phase 2 | Palmar hyperhidrosis | [3] | |
| 2 | 18-MC | Drug Info | Phase 1 | Substance use disorder | [4] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | Levopropoxyphene Napsylate Anhydrous | Drug Info | [1] | |||
| Antagonist | [+] 2 Antagonist drugs | + | ||||
| 1 | TC-5214 | Drug Info | [3] | |||
| 2 | 18-MC | Drug Info | [4] | |||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Nicotine | Ligand Info | |||||
| Structure Description | Human alpha3beta4 nicotinic acetylcholine receptor in complex with nicotine | PDB:6PV7 | ||||
| Method | Electron microscopy | Resolution | 3.34 Å | Mutation | No | [5] |
| PDB Sequence |
SEAEHRLFER
10 LFEDYNEIIR20 PVANVSDPVI30 IHFEVSMSQL40 VKVDEVNQIM50 ETNLWLKQIW 60 NDYKLKWNPS70 DYGGAEFMRV80 PAQKIWKPDI90 VLYNNAVGDF100 QVDDKTKALL 110 KYTGEVTWIP120 PAIFKSSCKI130 DVTYFPFDYQ140 NCTMKFGSWS150 YDKAKIDLVL 160 IGSSMNLKDY170 WESGEWAIIK180 APGYKHDIKY190 NCCEEIYPDI200 TYSLYIRRLP 210 LFYTINLIIP220 CLLISFLTVL230 VFYLPSDCGE240 KVTLCISVLL250 SLTVFLLVIT 260 ETIPSTSLVI270 PLIGEYLLFT280 MIFVTLSIVI290 TVFVLNVHYR300 TPTTHTMPSW 310 VKTVFLNLLP320 RVMFMTRIKE412 AIQSVKYIAE422 NMKAQNEAKE432 IQDDWKYVAM 442 VIDRIFLWVF452 TLVCILGTAG462 LFLQPLM
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| Ligand Name: Cholesterol hemisuccinate | Ligand Info | |||||
| Structure Description | Human alpha3beta4 nicotinic acetylcholine receptor in complex with nicotine | PDB:6PV7 | ||||
| Method | Electron microscopy | Resolution | 3.34 Å | Mutation | No | [5] |
| PDB Sequence |
SEAEHRLFER
10 LFEDYNEIIR20 PVANVSDPVI30 IHFEVSMSQL40 VKVDEVNQIM50 ETNLWLKQIW 60 NDYKLKWNPS70 DYGGAEFMRV80 PAQKIWKPDI90 VLYNNAVGDF100 QVDDKTKALL 110 KYTGEVTWIP120 PAIFKSSCKI130 DVTYFPFDYQ140 NCTMKFGSWS150 YDKAKIDLVL 160 IGSSMNLKDY170 WESGEWAIIK180 APGYKHDIKY190 NCCEEIYPDI200 TYSLYIRRLP 210 LFYTINLIIP220 CLLISFLTVL230 VFYLPSDCGE240 KVTLCISVLL250 SLTVFLLVIT 260 ETIPSTSLVI270 PLIGEYLLFT280 MIFVTLSIVI290 TVFVLNVHYR300 TPTTHTMPSW 310 VKTVFLNLLP320 RVMFMTRIKE412 AIQSVKYIAE422 NMKAQNEAKE432 IQDDWKYVAM 442 VIDRIFLWVF452 TLVCILGTAG462 LFLQPLM
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| 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 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 3 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 4 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 5 | Agonist Selectivity and Ion Permeation in the Alpha3beta4 Ganglionic Nicotinic Receptor. Neuron. 2019 Nov 6;104(3):501-511.e6. | |||||
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