Reaction Details |
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Target | ATP-binding cassette sub-family C member 8/ATP-sensitive inward rectifier potassium channel 11 |
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Ligand | BDBM50118351 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_206297 (CHEMBL810542) |
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IC50 | 10800±n/a nM |
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Citation | Nielsen, FE; Bodvarsdottir, TB; Worsaae, A; MacKay, P; Stidsen, CE; Boonen, HC; Pridal, L; Arkhammar, PO; Wahl, P; Ynddal, L; Junager, F; Dragsted, N; Tagmose, TM; Mogensen, JP; Koch, A; Treppendahl, SP; Hansen, JB 6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells. J Med Chem45:4171-87 (2002) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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ATP-binding cassette sub-family C member 8/ATP-sensitive inward rectifier potassium channel 11 |
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Name: | ATP-binding cassette sub-family C member 8/ATP-sensitive inward rectifier potassium channel 11 |
Synonyms: | Potassium channel, inwardly rectifying, subfamily J, member 11/Sulfonylurea receptor 1 | Sulfonylurea receptor 1, Kir6.2 |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of EBI is 39363 |
Components: | This complex has 2 components. |
Component 1 |
Name: | ATP-binding cassette sub-family C member 8 |
Synonyms: | ABCC8 | ABCC8_HUMAN | ATP-binding cassette sub-family C member 8 | ATP-binding cassette transporter sub-family C member 8 | HRINS | K-ATP channels | SUR | SUR1 | Sulfonylurea receptor 1 | Sulfonylurea receptors |
Type: | PROTEIN |
Mol. Mass.: | 177013.37 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_1436733 |
Residue: | 1581 |
Sequence: | MPLAFCGSENHSAAYRVDQGVLNNGCFVDALNVVPHVFLLFITFPILFIGWGSQSSKVHI
HHSTWLHFPGHNLRWILTFMLLFVLVCEIAEGILSDGVTESHHLHLYMPAGMAFMAAVTS
VVYYHNIETSNFPKLLIALLVYWTLAFITKTIKFVKFLDHAIGFSQLRFCLTGLLVILYG
MLLLVEVNVIRVRRYIFFKTPREVKPPEDLQDLGVRFLQPFVNLLSKGTYWWMNAFIKTA
HKKPIDLRAIGKLPIAMRALTNYQRLCEAFDAQVRKDIQGTQGARAIWQALSHAFGRRLV
LSSTFRILADLLGFAGPLCIFGIVDHLGKENDVFQPKTQFLGVYFVSSQEFLANAYVLAV
LLFLALLLQRTFLQASYYVAIETGINLRGAIQTKIYNKIMHLSTSNLSMGEMTAGQICNL
VAIDTNQLMWFFFLCPNLWAMPVQIIVGVILLYYILGVSALIGAAVIILLAPVQYFVATK
LSQAQRSTLEYSNERLKQTNEMLRGIKLLKLYAWENIFRTRVETTRRKEMTSLRAFAIYT
SISIFMNTAIPIAAVLITFVGHVSFFKEADFSPSVAFASLSLFHILVTPLFLLSSVVRST
VKALVSVQKLSEFLSSAEIREEQCAPHEPTPQGPASKYQAVPLRVVNRKRPAREDCRGLT
GPLQSLVPSADGDADNCCVQIMGGYFTWTPDGIPTLSNITIRIPRGQLTMIVGQVGCGKS
SLLLAALGEMQKVSGAVFWSSLPDSEIGEDPSPERETATDLDIRKRGPVAYASQKPWLLN
ATVEENIIFESPFNKQRYKMVIEACSLQPDIDILPHGDQTQIGERGINLSGGQRQRISVA
RALYQHANVVFLDDPFSALDIHLSDHLMQAGILELLRDDKRTVVLVTHKLQYLPHADWII
AMKDGTIQREGTLKDFQRSECQLFEHWKTLMNRQDQELEKETVTERKATEPPQGLSRAMS
SRDGLLQDEEEEEEEAAESEEDDNLSSMLHQRAEIPWRACAKYLSSAGILLLSLLVFSQL
LKHMVLVAIDYWLAKWTDSALTLTPAARNCSLSQECTLDQTVYAMVFTVLCSLGIVLCLV
TSVTVEWTGLKVAKRLHRSLLNRIILAPMRFFETTPLGSILNRFSSDCNTIDQHIPSTLE
CLSRSTLLCVSALAVISYVTPVFLVALLPLAIVCYFIQKYFRVASRDLQQLDDTTQLPLL
SHFAETVEGLTTIRAFRYEARFQQKLLEYTDSNNIASLFLTAANRWLEVRMEYIGACVVL
IAAVTSISNSLHRELSAGLVGLGLTYALMVSNYLNWMVRNLADMELQLGAVKRIHGLLKT
EAESYEGLLAPSLIPKNWPDQGKIQIQNLSVRYDSSLKPVLKHVNALIAPGQKIGICGRT
GSGKSSFSLAFFRMVDTFEGHIIIDGIDIAKLPLHTLRSRLSIILQDPVLFSGTIRFNLD
PERKCSDSTLWEALEIAQLKLVVKALPGGLDAIITEGGENFSQGQRQLFCLARAFVRKTS
IFIMDEATASIDMATENILQKVVMTAFADRTVVTIAHRVHTILSADLVIVLKRGAILEFD
KPEKLLSRKDSVFASFVRADK
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Component 2 |
Name: | ATP-sensitive inward rectifier potassium channel 11 |
Synonyms: | ATP-sensitive inward rectifier potassium channel 11 | IKATP | Inward rectifier K(+) channel Kir6.2 | KCJ11_HUMAN | KCNJ11 | Potassium channel, inwardly rectifying subfamily J member 11 | Potassium channel, inwardly rectifying, subfamily J, member 11 | Sulfonylurea receptor 1, Kir6.2 | Sulfonylurea receptor 2, Kir6.2 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 43549.41 |
Organism: | Homo sapiens (Human) |
Description: | Potassium channel (ATP modulatory) 0 0::Q14654 |
Residue: | 390 |
Sequence: | MLSRKGIIPEEYVLTRLAEDPAEPRYRARQRRARFVSKKGNCNVAHKNIREQGRFLQDVF
TTLVDLKWPHTLLIFTMSFLCSWLLFAMAWWLIAFAHGDLAPSEGTAEPCVTSIHSFSSA
FLFSIEVQVTIGFGGRMVTEECPLAILILIVQNIVGLMINAIMLGCIFMKTAQAHRRAET
LIFSKHAVIALRHGRLCFMLRVGDLRKSMIISATIHMQVVRKTTSPEGEVVPLHQVDIPM
ENGVGGNSIFLVAPLIIYHVIDANSPLYDLAPSDLHHHQDLEIIVILEGVVETTGITTQA
RTSYLADEILWGQRFVPIVAEEDGRYSVDYSKFGNTIKVPTPLCTARQLDEDHSLLEALT
LASARGPLRKRSVPMAKAKPKFSISPDSLS
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Component 3 |
Name: | ATP-binding cassette sub-family C member 8 |
Synonyms: | ABCC8 | ABCC8_HUMAN | ATP-binding cassette sub-family C member 8 | ATP-binding cassette transporter sub-family C member 8 | HRINS | K-ATP channels | SUR | SUR1 | Sulfonylurea receptor 1 | Sulfonylurea receptors |
Type: | PROTEIN |
Mol. Mass.: | 177013.37 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_1436733 |
Residue: | 1581 |
Sequence: | MPLAFCGSENHSAAYRVDQGVLNNGCFVDALNVVPHVFLLFITFPILFIGWGSQSSKVHI
HHSTWLHFPGHNLRWILTFMLLFVLVCEIAEGILSDGVTESHHLHLYMPAGMAFMAAVTS
VVYYHNIETSNFPKLLIALLVYWTLAFITKTIKFVKFLDHAIGFSQLRFCLTGLLVILYG
MLLLVEVNVIRVRRYIFFKTPREVKPPEDLQDLGVRFLQPFVNLLSKGTYWWMNAFIKTA
HKKPIDLRAIGKLPIAMRALTNYQRLCEAFDAQVRKDIQGTQGARAIWQALSHAFGRRLV
LSSTFRILADLLGFAGPLCIFGIVDHLGKENDVFQPKTQFLGVYFVSSQEFLANAYVLAV
LLFLALLLQRTFLQASYYVAIETGINLRGAIQTKIYNKIMHLSTSNLSMGEMTAGQICNL
VAIDTNQLMWFFFLCPNLWAMPVQIIVGVILLYYILGVSALIGAAVIILLAPVQYFVATK
LSQAQRSTLEYSNERLKQTNEMLRGIKLLKLYAWENIFRTRVETTRRKEMTSLRAFAIYT
SISIFMNTAIPIAAVLITFVGHVSFFKEADFSPSVAFASLSLFHILVTPLFLLSSVVRST
VKALVSVQKLSEFLSSAEIREEQCAPHEPTPQGPASKYQAVPLRVVNRKRPAREDCRGLT
GPLQSLVPSADGDADNCCVQIMGGYFTWTPDGIPTLSNITIRIPRGQLTMIVGQVGCGKS
SLLLAALGEMQKVSGAVFWSSLPDSEIGEDPSPERETATDLDIRKRGPVAYASQKPWLLN
ATVEENIIFESPFNKQRYKMVIEACSLQPDIDILPHGDQTQIGERGINLSGGQRQRISVA
RALYQHANVVFLDDPFSALDIHLSDHLMQAGILELLRDDKRTVVLVTHKLQYLPHADWII
AMKDGTIQREGTLKDFQRSECQLFEHWKTLMNRQDQELEKETVTERKATEPPQGLSRAMS
SRDGLLQDEEEEEEEAAESEEDDNLSSMLHQRAEIPWRACAKYLSSAGILLLSLLVFSQL
LKHMVLVAIDYWLAKWTDSALTLTPAARNCSLSQECTLDQTVYAMVFTVLCSLGIVLCLV
TSVTVEWTGLKVAKRLHRSLLNRIILAPMRFFETTPLGSILNRFSSDCNTIDQHIPSTLE
CLSRSTLLCVSALAVISYVTPVFLVALLPLAIVCYFIQKYFRVASRDLQQLDDTTQLPLL
SHFAETVEGLTTIRAFRYEARFQQKLLEYTDSNNIASLFLTAANRWLEVRMEYIGACVVL
IAAVTSISNSLHRELSAGLVGLGLTYALMVSNYLNWMVRNLADMELQLGAVKRIHGLLKT
EAESYEGLLAPSLIPKNWPDQGKIQIQNLSVRYDSSLKPVLKHVNALIAPGQKIGICGRT
GSGKSSFSLAFFRMVDTFEGHIIIDGIDIAKLPLHTLRSRLSIILQDPVLFSGTIRFNLD
PERKCSDSTLWEALEIAQLKLVVKALPGGLDAIITEGGENFSQGQRQLFCLARAFVRKTS
IFIMDEATASIDMATENILQKVVMTAFADRTVVTIAHRVHTILSADLVIVLKRGAILEFD
KPEKLLSRKDSVFASFVRADK
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BDBM50118351 |
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n/a |
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Name | BDBM50118351 |
Synonyms: | (2-Chloro-7,7-dioxo-4,7-dihydro-1,7lambda*6*-dithia-4,6-diaza-inden-5-yl)-(1-methyl-cyclobutyl)-amine | 6-chloro-3-(1-methylcyclobutyl)-amino-4H-thieno[3,2-e]-1,2,4-thiadiazine1,1-dioxide | CHEMBL134168 |
Type | Small organic molecule |
Emp. Form. | C10H12ClN3O2S2 |
Mol. Mass. | 305.804 |
SMILES | CC1(CCC1)NC1=Nc2cc(Cl)sc2S(=O)(=O)N1 |t:7| |
Structure |
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