Target Binding Site Detail
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T93266 | Target Info | |||
| Target Name | Hyperpolarization cyclic nucleotide-gated channel 1 (HCN1) | ||||
| Synonyms | Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1; Brain cyclic nucleotide-gated channel 1; BCNG1; BCNG-1 | ||||
| Target Type | Literature-reported Target | ||||
| Gene Name | HCN1 | ||||
| Biochemical Class | Voltage-gated ion channel | ||||
| UniProt ID | |||||
| Ligand General Information | Top | ||||
|---|---|---|---|---|---|
| Ligand Name | [3H]cAMP | Ligand Info | |||
| Canonical SMILES | C1C2C(C(C(O2)N3C=NC4=C(N=CN=C43)N)O)OP(=O)(O1)O | ||||
| InChI | 1S/C10H12N5O6P/c11-8-5-9(13-2-12-8)15(3-14-5)10-6(16)7-4(20-10)1-19-22(17,18)21-7/h2-4,6-7,10,16H,1H2,(H,17,18)(H2,11,12,13)/t4-,6-,7-,10-/m1/s1 | ||||
| InChIKey | IVOMOUWHDPKRLL-KQYNXXCUSA-N | ||||
| PubChem Compound ID | 6076 | ||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| PDB ID: 6UQF Human HCN1 channel in a hyperpolarized conformation | ||||||
| Method | Electron microscopy | Resolution | 3.04 Å | Mutation | No | [1] |
| PDB Sequence |
MQRQFTSMLQ
103 PGVNKFSLRM113 FGSQKAVEKE123 QERVKTAGFW133 IIHPYSDFRF143 YWDLIMLIMM 153 VGNLVIIPVG163 ITFFTEQTTT173 PWIIFNVASD183 TVCLLDLIMN193 FRTGTVNEDS 203 SEIILDPKVI213 KMNYLKSWFV223 VDFISSIPVD233 YIFLIVERAL254 RIVRFTKILC 264 LLRLLRLSRL274 IRYIHQWEEI284 FHMTYDLASA294 VVRIFNLIGM304 MLLLCHWDGC 314 LQFLVPLLQD324 FPPDCWVSLN334 EMVNDSWGKQ344 YSYALFKAMS354 HMLCIGYGAQ 364 APVSMSDLWI374 TMLSMIVGAT384 CYAMFVGHAT394 ALIQSLDSSR404 RQYQEKYKQV 414 EQYMSFHKLP424 ADMRQKIHDY434 YEHRYQGKIF444 DEENILNELN454 DPLREEIVNF 464 NCRKLVATMP474 LFANADPNFV484 TAMLSKLRFE494 VFQPGDYIIR504 EGAVGKKMYF 514 IQHGVAGVIT524 KSSKEMKLTD534 GSYFGEICLL544 TKGRRTASVR554 ADTYCRLYSL 564 SVDNFNEVLE574 EYPMMRRAFE584 TVAIDRLDRI594 GKKNSILLQK604 FQKDLNTGVF 614 NNQENEILKQ624 IVKHDREMVQ634 A
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| PDB ID: 5U6P Structure of the human HCN1 hyperpolarization-activated cyclic nucleotide-gated ion channel in complex with cAMP | ||||||
| Method | Electron microscopy | Resolution | 3.51 Å | Mutation | No | [2] |
| PDB Sequence |
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ILE503[A]
4.258
VAL522[A]
4.549
MET530[A]
3.254
LEU532[A]
4.172
TYR537[A]
4.716
PHE538[A]
3.500
GLY539[A]
2.733
GLU540[A]
3.374
ILE541[A]
3.486
CYS542[A]
3.112
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| PDB ID: 6UQG Human HCN1 channel Y289D mutant | ||||||
| Method | Electron microscopy | Resolution | 3.54 Å | Mutation | Yes | [1] |
| PDB Sequence |
MQRQFTSMLQ
103 PGVNKFSLRM113 FGSQKAVEKE123 QERVKTAGFW133 IIHPYSDFRF143 YWDLIMLIMM 153 VGNLVIIPVG163 ITFFTEQTTT173 PWIIFNVASD183 TVFLLDLIMN193 FRTGTVNSSE 205 IILDPKVIKM215 NYLKSWFVVD225 FISSIPVDYI235 FLIVEKGALR255 IVRFTKILSL 265 LRLLRLSRLI275 RYIHQWEEIF285 HMTDDLASAV295 VRIFNLIGMM305 LLLCHWDGCL 315 QFLVPLLQDF325 PPDCWVSLNE335 MVNDSWGKQY345 SYALFKAMSH355 MLCIGYGAQA 365 PVSMSDLWIT375 MLSMIVGATC385 YAMFVGHATA395 LIQSLDSSRR405 QYQEKYKQVE 415 QYMSFHKLPA425 DMRQKIHDYY435 EHRYQGKIFD445 EENILNELND455 PLREEIVNFN 465 CRKLVATMPL475 FANADPNFVT485 AMLSKLRFEV495 FQPGDYIIRE505 GAVGKKMYFI 515 QHGVAGVITK525 SSKEMKLTDG535 SYFGEICLLT545 KGRRTASVRA555 DTYCRLYSLS 565 VDNFNEVLEE575 YPMMRRAFET585 VAIDRLDRIG595 KKNSILLQKF605 QKDLNTGVFN 615 NQENEILKQI625 VKHDREMVQA635
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Voltage Sensor Movements during Hyperpolarization in the HCN Channel. Cell. 2019 Dec 12;179(7):1582-1589.e7. | ||||
| REF 2 | Structures of the Human HCN1 Hyperpolarization-Activated Channel. Cell. 2017 Jan 12;168(1-2):111-120.e11. | ||||
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