Target Binding Site Detail
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T93798 | Target Info | |||
| Target Name | Cyclic nucleotide-gated channel alpha-1 (CNGA1) | ||||
| Synonyms | cGMP-gated cation channel alpha-1; Rod photoreceptor cGMP-gated channel subunit alpha; Cyclic nucleotide-gated channel, photoreceptor; Cyclic nucleotide-gated cation channel 1; CNG1; CNG-1; CNG channel alpha-1; CNCG1; CNCG | ||||
| Target Type | Clinical trial Target | ||||
| Gene Name | CNGA1 | ||||
| UniProt ID | |||||
| Ligand General Information | Top | ||||
|---|---|---|---|---|---|
| Ligand Name | Cyclic Guanosine Monophosphate | Ligand Info | |||
| Canonical SMILES | C1C2C(C(C(O2)N3C=NC4=C3N=C(NC4=O)N)O)OP(=O)(O1)O | ||||
| InChI | 1S/C10H12N5O7P/c11-10-13-7-4(8(17)14-10)12-2-15(7)9-5(16)6-3(21-9)1-20-23(18,19)22-6/h2-3,5-6,9,16H,1H2,(H,18,19)(H3,11,13,14,17)/t3-,5-,6-,9-/m1/s1 | ||||
| InChIKey | ZOOGRGPOEVQQDX-UUOKFMHZSA-N | ||||
| PubChem Compound ID | 135398570 | ||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| PDB ID: 7LG1 Cryo-EM structure of human cGMP-bound CNGA1_E365Q channel in Na+/Ca2+ | ||||||
| Method | Electron microscopy | Resolution | 2.70 Å | Mutation | Yes | [1] |
| PDB Sequence |
VVIDPSGNTY
165 YNWLFCITLP175 VMYNWTMVIA185 RACFDELQSD195 YLEYWLILDY205 VSDIVYLIDM 215 FVRTRTGYLE225 QGLLVKEELK235 LINKYKSNLQ245 FKLDVLSLIP255 TDLLYFKLGW 265 NYPEIRLNRL275 LRFSRMFEFF285 QRTETRTNYP295 NIFRISNLVM305 YIVIIIHWNA 315 CVFYSISKAI325 GFGNDTWVYP335 DINDPEFGRL345 ARKYVYSLYW355 STLTLTTIGQ 365 TPPPVRDSEY375 VFVVVDFLIG385 VLIFATIVGN395 IGSMISNMNA405 ARAEFQARID 415 AIKQYMHFRN425 VSKDMEKRVI435 KWFDYLWTNK445 KTVDEKEVLK455 YLPDKLRAEI 465 AINVHLDTLK475 KVRIFADCEA485 GLLVELVLKL495 QPQVYSPGDY505 ICKKGDIGRE 515 MYIIKEGKLA525 VVADDGVTQF535 VVLSDGSYFG545 EISILNIKGS555 KAGNRRTANI 565 KSIGYSDLFC575 LSKDDLMEAL585 TEYPDAKTML595 EEKGKQILMK605 |
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| PDB ID: 7RHJ Cryo-EM structure of human rod CNGA1/B1 channel in L-cis-Diltiazem-blocked open state | ||||||
| Method | Electron microscopy | Resolution | 2.88 Å | Mutation | No | [2] |
| PDB Sequence |
VVIDPSGNTY
165 YNWLFCITLP175 VMYNWTMVIA185 RACFDELQSD195 YLEYWLILDY205 VSDIVYLIDM 215 FVRTRTGYLE225 QGLLVKEELK235 LINKYKSNLQ245 FKLDVLSLIP255 TDLLYFKLGW 265 NYPEIRLNRL275 LRFSRMFEFF285 QRTETRTNYP295 NIFRISNLVM305 YIVIIIHWNA 315 CVFYSISKAI325 GFGNDTWVYP335 DINDPEFGRL345 ARKYVYSLYW355 STLTLTTIGE 365 TPPPVRDSEY375 VFVVVDFLIG385 VLIFATIVGN395 IGSMISNMNA405 ARAEFQARID 415 AIKQYMHFRN425 VSKDMEKRVI435 KWFDYLWTNK445 KTVDEKEVLK455 YLPDKLRAEI 465 AINVHLDTLK475 KVRIFADCEA485 GLLVELVLKL495 QPQVYSPGDY505 ICKKGDIGRE 515 MYIIKEGKLA525 VVADDGVTQF535 VVLSDGSYFG545 EISILNIKGS555 KAGNRRTANI 565 KSIGYSDLFC575 LSKDDLMEAL585 TEYPDAKTML595 EEKGKQILMK605 |
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| PDB ID: 7LFW Cryo-EM structure of human cGMP-bound open CNGA1 channel in K+/Ca2+ | ||||||
| Method | Electron microscopy | Resolution | 2.90 Å | Mutation | No | [1] |
| PDB Sequence |
VVIDPSGNTY
165 YNWLFCITLP175 VMYNWTMVIA185 RACFDELQSD195 YLEYWLILDY205 VSDIVYLIDM 215 FVRTRTGYLE225 QGLLVKEELK235 LINKYKSNLQ245 FKLDVLSLIP255 TDLLYFKLGW 265 NYPEIRLNRL275 LRFSRMFEFF285 QRTETRTNYP295 NIFRISNLVM305 YIVIIIHWNA 315 CVFYSISKAI325 GFGNDTWVYP335 DINDPEFGRL345 ARKYVYSLYW355 STLTLTTIGE 365 TPPPVRDSEY375 VFVVVDFLIG385 VLIFATIVGN395 IGSMISNMNA405 ARAEFQARID 415 AIKQYMHFRN425 VSKDMEKRVI435 KWFDYLWTNK445 KTVDEKEVLK455 YLPDKLRAEI 465 AINVHLDTLK475 KVRIFADCEA485 GLLVELVLKL495 QPQVYSPGDY505 ICKKGDIGRE 515 MYIIKEGKLA525 VVADDGVTQF535 VVLSDGSYFG545 EISILNIKGS555 KAGNRRTANI 565 KSIGYSDLFC575 LSKDDLMEAL585 TEYPDAKTML595 EEKGKQILMK605 |
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| PDB ID: 7LFX Cryo-EM structure of human cGMP-bound open CNGA1 channel in Na+/Ca2+ | ||||||
| Method | Electron microscopy | Resolution | 3.10 Å | Mutation | No | [1] |
| PDB Sequence |
VVIDPSGNTY
165 YNWLFCITLP175 VMYNWTMVIA185 RACFDELQSD195 YLEYWLILDY205 VSDIVYLIDM 215 FVRTRTGYLE225 QGLLVKEELK235 LINKYKSNLQ245 FKLDVLSLIP255 TDLLYFKLGW 265 NYPEIRLNRL275 LRFSRMFEFF285 QRTETRTNYP295 NIFRISNLVM305 YIVIIIHWNA 315 CVFYSISKAI325 GFGNDTWVYP335 DINDPEFGRL345 ARKYVYSLYW355 STLTLTTIGE 365 TPPPVRDSEY375 VFVVVDFLIG385 VLIFATIVGN395 IGSMISNMNA405 ARAEFQARID 415 AIKQYMHFRN425 VSKDMEKRVI435 KWFDYLWTNK445 KTVDEKEVLK455 YLPDKLRAEI 465 AINVHLDTLK475 KVRIFADCEA485 GLLVELVLKL495 QPQVYSPGDY505 ICKKGDIGRE 515 MYIIKEGKLA525 VVADDGVTQF535 VVLSDGSYFG545 EISILNIKGS555 KAGNRRTANI 565 KSIGYSDLFC575 LSKDDLMEAL585 TEYPDAKTML595 EEKGKQILMK605 |
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .PCG or .PCG2 or .PCG3 or :3PCG;style chemicals stick;color identity;select .A:507 or .A:526 or .A:536 or .A:538 or .A:543 or .A:544 or .A:545 or .A:546 or .A:547 or .A:548 or .A:560 or .A:561 or .A:562 or .A:563 or .A:565 or .A:602; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| PDB ID: 7RHK Cryo-EM structure of human rod CNGA1/B1 channel in L-cis-Diltiazem-trapped closed state | ||||||
| Method | Electron microscopy | Resolution | 3.27 Å | Mutation | No | [2] |
| PDB Sequence |
VVIDPSGNTY
165 YNWLFCITLP175 VMYNWTMVIA185 RACFDELQSD195 YLEYWLILDY205 VSDIVYLIDM 215 FVRTRTGYLE225 QGLLVKEELK235 LINKYKSNLQ245 FKLDVLSLIP255 TDLLYFKLGW 265 NYPEIRLNRL275 LRFSRMFEFF285 QRTETRTNYP295 NIFRISNLVM305 YIVIIIHWNA 315 CVFYSISKAI325 GFGNDTWVYP335 DINDPEFGRL345 ARKYVYSLYW355 STLTLTTIGE 365 TPPPVRDSEY375 VFVVVDFLIG385 VLIFATIVGN395 IGSMISNMNA405 ARAEFQARID 415 AIKQYMHFRN425 VSKDMEKRVI435 KWFDYLWTNK445 KTVDEKEVLK455 YLPDKLRAEI 465 AINVHLDTLK475 KVRIFADCEA485 GLLVELVLKL495 QPQVYSPGDY505 ICKKGDIGRE 515 MYIIKEGKLA525 VVADDGVTQF535 VVLSDGSYFG545 EISILNIKGS555 KAGNRRTANI 565 KSIGYSDLFC575 LSKDDLMEAL585 TEYPDAKTML595 EEKGKQILMK605 |
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .PCG or .PCG2 or .PCG3 or :3PCG;style chemicals stick;color identity;select .C:507 or .C:526 or .C:535 or .C:536 or .C:538 or .C:544 or .C:545 or .C:546 or .C:547 or .C:548 or .C:560 or .C:561 or .C:562 or .C:563 or .C:565; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| PDB ID: 7RHH Cryo-EM structure of human rod CNGA1/B1 channel in cGMP-bound openI state | ||||||
| Method | Electron microscopy | Resolution | 3.31 Å | Mutation | No | [2] |
| PDB Sequence |
VVIDPSGNTY
165 YNWLFCITLP175 VMYNWTMVIA185 RACFDELQSD195 YLEYWLILDY205 VSDIVYLIDM 215 FVRTRTGYLE225 QGLLVKEELK235 LINKYKSNLQ245 FKLDVLSLIP255 TDLLYFKLGW 265 NYPEIRLNRL275 LRFSRMFEFF285 QRTETRTNYP295 NIFRISNLVM305 YIVIIIHWNA 315 CVFYSISKAI325 GFGNDTWVYP335 DINDPEFGRL345 ARKYVYSLYW355 STLTLTTIGE 365 TPPPVRDSEY375 VFVVVDFLIG385 VLIFATIVGN395 IGSMISNMNA405 ARAEFQARID 415 AIKQYMHFRN425 VSKDMEKRVI435 KWFDYLWTNK445 KTVDEKEVLK455 YLPDKLRAEI 465 AINVHLDTLK475 KVRIFADCEA485 GLLVELVLKL495 QPQVYSPGDY505 ICKKGDIGRE 515 MYIIKEGKLA525 VVADDGVTQF535 VVLSDGSYFG545 EISILNIKGS555 KAGNRRTANI 565 KSIGYSDLFC575 LSKDDLMEAL585 TEYPDAKTML595 EEKGKQILMK605 |
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .PCG or .PCG2 or .PCG3 or :3PCG;style chemicals stick;color identity;select .A:507 or .A:526 or .A:538 or .A:543 or .A:544 or .A:545 or .A:546 or .A:547 or .A:548 or .A:560 or .A:561 or .A:562 or .A:563 or .A:564 or .A:565 or .A:602 or .A:605; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
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| PDB ID: 7RHI Cryo-EM structure of human rod CNGA1/B1 channel in cGMP-bound openII state | ||||||
| Method | Electron microscopy | Resolution | 3.31 Å | Mutation | No | [2] |
| PDB Sequence |
VVIDPSGNTY
165 YNWLFCITLP175 VMYNWTMVIA185 RACFDELQSD195 YLEYWLILDY205 VSDIVYLIDM 215 FVRTRTGYLE225 QGLLVKEELK235 LINKYKSNLQ245 FKLDVLSLIP255 TDLLYFKLGW 265 NYPEIRLNRL275 LRFSRMFEFF285 QRTETRTNYP295 NIFRISNLVM305 YIVIIIHWNA 315 CVFYSISKAI325 GFGNDTWVYP335 DINDPEFGRL345 ARKYVYSLYW355 STLTLTTIGE 365 TPPPVRDSEY375 VFVVVDFLIG385 VLIFATIVGN395 IGSMISNMNA405 ARAEFQARID 415 AIKQYMHFRN425 VSKDMEKRVI435 KWFDYLWTNK445 KTVDEKEVLK455 YLPDKLRAEI 465 AINVHLDTLK475 KVRIFADCEA485 GLLVELVLKL495 QPQVYSPGDY505 ICKKGDIGRE 515 MYIIKEGKLA525 VVADDGVTQF535 VVLSDGSYFG545 EISILNIKGS555 KAGNRRTANI 565 KSIGYSDLFC575 LSKDDLMEAL585 TEYPDAKTML595 EEKGKQILMK605 |
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .PCG or .PCG2 or .PCG3 or :3PCG;style chemicals stick;color identity;select .A:507 or .A:526 or .A:538 or .A:544 or .A:545 or .A:546 or .A:547 or .A:548 or .A:560 or .A:561 or .A:562 or .A:563 or .A:565 or .A:602; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
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| PDB ID: 7LFY Cryo-EM structure of human cGMP-bound open CNGA1 channel in Na+ | ||||||
| Method | Electron microscopy | Resolution | 3.60 Å | Mutation | No | [1] |
| PDB Sequence |
VVIDPSGNTY
165 YNWLFCITLP175 VMYNWTMVIA185 RACFDELQSD195 YLEYWLILDY205 VSDIVYLIDM 215 FVRTRTGYLE225 QGLLVKEELK235 LINKYKSNLQ245 FKLDVLSLIP255 TDLLYFKLGW 265 NYPEIRLNRL275 LRFSRMFEFF285 QRTETRTNYP295 NIFRISNLVM305 YIVIIIHWNA 315 CVFYSISKAI325 GFGNDTWVYP335 DINDPEFGRL345 ARKYVYSLYW355 STLTLTTIGE 365 TPPPVRDSEY375 VFVVVDFLIG385 VLIFATIVGN395 IGSMISNMNA405 ARAEFQARID 415 AIKQYMHFRN425 VSKDMEKRVI435 KWFDYLWTNK445 KTVDEKEVLK455 YLPDKLRAEI 465 AINVHLDTLK475 KVRIFADCEA485 GLLVELVLKL495 QPQVYSPGDY505 ICKKGDIGRE 515 MYIIKEGKLA525 VVADDGVTQF535 VVLSDGSYFG545 EISILNIKGS555 KAGNRRTANI 565 KSIGYSDLFC575 LSKDDLMEAL585 TEYPDAKTML595 EEKGKQILMK605 |
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .PCG or .PCG2 or .PCG3 or :3PCG;style chemicals stick;color identity;select .A:507 or .A:526 or .A:536 or .A:538 or .A:543 or .A:544 or .A:545 or .A:546 or .A:547 or .A:548 or .A:560 or .A:561 or .A:562 or .A:563 or .A:565 or .A:602; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structural mechanisms of gating and selectivity of human rod CNGA1 channel. Neuron. 2021 Apr 21;109(8):1302-1313.e4. | ||||
| REF 2 | Structural mechanisms of assembly, permeation, gating, and pharmacology of native human rod CNG channel. Neuron. 2022 Jan 5;110(1):86-95.e5. | ||||
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