Target
ATP-binding cassette sub-family C member 8/ATP-sensitive inward rectifier potassium channel 11
Ligand
BDBM50118359
Substrate
n/a
Meas. Tech.
ChEMBL_373849 (CHEMBL864945)
IC50
696000±n/a nM
Citation
 Nielsen, FEEbdrup, SJensen, AFYnddal, LBodvarsdottir, TBStidsen, CWorsaae, ABoonen, HCArkhammar, POFremming, TWahl, PKornø, HTHansen, JB New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells. J Med Chem 49:4127-39 (2006) [PubMed]  Article 
Target
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:
MPLAFCGSENHSAAYRVDQGVLNNGCFVDALNVVPHVFLLFITFPILFIGWGSQSSKVHIHHSTWLHFPGHNLRWILTFMLLFVLVCEIAEGILSDGVTESHHLHLYMPAGMAFMAAVTSVVYYHNIETSNFPKLLIALLVYWTLAFITKTIKFVKFLDHAIGFSQLRFCLTGLLVILYGMLLLVEVNVIRVRRYIFFKTPREVKPPEDLQDLGVRFLQPFVNLLSKGTYWWMNAFIKTAHKKPIDLRAIGKLPIAMRALTNYQRLCEAFDAQVRKDIQGTQGARAIWQALSHAFGRRLVLSSTFRILADLLGFAGPLCIFGIVDHLGKENDVFQPKTQFLGVYFVSSQEFLANAYVLAVLLFLALLLQRTFLQASYYVAIETGINLRGAIQTKIYNKIMHLSTSNLSMGEMTAGQICNLVAIDTNQLMWFFFLCPNLWAMPVQIIVGVILLYYILGVSALIGAAVIILLAPVQYFVATKLSQAQRSTLEYSNERLKQTNEMLRGIKLLKLYAWENIFRTRVETTRRKEMTSLRAFAIYTSISIFMNTAIPIAAVLITFVGHVSFFKEADFSPSVAFASLSLFHILVTPLFLLSSVVRSTVKALVSVQKLSEFLSSAEIREEQCAPHEPTPQGPASKYQAVPLRVVNRKRPAREDCRGLTGPLQSLVPSADGDADNCCVQIMGGYFTWTPDGIPTLSNITIRIPRGQLTMIVGQVGCGKSSLLLAALGEMQKVSGAVFWSSLPDSEIGEDPSPERETATDLDIRKRGPVAYASQKPWLLNATVEENIIFESPFNKQRYKMVIEACSLQPDIDILPHGDQTQIGERGINLSGGQRQRISVARALYQHANVVFLDDPFSALDIHLSDHLMQAGILELLRDDKRTVVLVTHKLQYLPHADWIIAMKDGTIQREGTLKDFQRSECQLFEHWKTLMNRQDQELEKETVTERKATEPPQGLSRAMSSRDGLLQDEEEEEEEAAESEEDDNLSSMLHQRAEIPWRACAKYLSSAGILLLSLLVFSQLLKHMVLVAIDYWLAKWTDSALTLTPAARNCSLSQECTLDQTVYAMVFTVLCSLGIVLCLVTSVTVEWTGLKVAKRLHRSLLNRIILAPMRFFETTPLGSILNRFSSDCNTIDQHIPSTLECLSRSTLLCVSALAVISYVTPVFLVALLPLAIVCYFIQKYFRVASRDLQQLDDTTQLPLLSHFAETVEGLTTIRAFRYEARFQQKLLEYTDSNNIASLFLTAANRWLEVRMEYIGACVVLIAAVTSISNSLHRELSAGLVGLGLTYALMVSNYLNWMVRNLADMELQLGAVKRIHGLLKTEAESYEGLLAPSLIPKNWPDQGKIQIQNLSVRYDSSLKPVLKHVNALIAPGQKIGICGRTGSGKSSFSLAFFRMVDTFEGHIIIDGIDIAKLPLHTLRSRLSIILQDPVLFSGTIRFNLDPERKCSDSTLWEALEIAQLKLVVKALPGGLDAIITEGGENFSQGQRQLFCLARAFVRKTSIFIMDEATASIDMATENILQKVVMTAFADRTVVTIAHRVHTILSADLVIVLKRGAILEFDKPEKLLSRKDSVFASFVRADK
  
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:
MLSRKGIIPEEYVLTRLAEDPAEPRYRARQRRARFVSKKGNCNVAHKNIREQGRFLQDVFTTLVDLKWPHTLLIFTMSFLCSWLLFAMAWWLIAFAHGDLAPSEGTAEPCVTSIHSFSSAFLFSIEVQVTIGFGGRMVTEECPLAILILIVQNIVGLMINAIMLGCIFMKTAQAHRRAETLIFSKHAVIALRHGRLCFMLRVGDLRKSMIISATIHMQVVRKTTSPEGEVVPLHQVDIPMENGVGGNSIFLVAPLIIYHVIDANSPLYDLAPSDLHHHQDLEIIVILEGVVETTGITTQARTSYLADEILWGQRFVPIVAEEDGRYSVDYSKFGNTIKVPTPLCTARQLDEDHSLLEALTLASARGPLRKRSVPMAKAKPKFSISPDSLS
  
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:
MPLAFCGSENHSAAYRVDQGVLNNGCFVDALNVVPHVFLLFITFPILFIGWGSQSSKVHIHHSTWLHFPGHNLRWILTFMLLFVLVCEIAEGILSDGVTESHHLHLYMPAGMAFMAAVTSVVYYHNIETSNFPKLLIALLVYWTLAFITKTIKFVKFLDHAIGFSQLRFCLTGLLVILYGMLLLVEVNVIRVRRYIFFKTPREVKPPEDLQDLGVRFLQPFVNLLSKGTYWWMNAFIKTAHKKPIDLRAIGKLPIAMRALTNYQRLCEAFDAQVRKDIQGTQGARAIWQALSHAFGRRLVLSSTFRILADLLGFAGPLCIFGIVDHLGKENDVFQPKTQFLGVYFVSSQEFLANAYVLAVLLFLALLLQRTFLQASYYVAIETGINLRGAIQTKIYNKIMHLSTSNLSMGEMTAGQICNLVAIDTNQLMWFFFLCPNLWAMPVQIIVGVILLYYILGVSALIGAAVIILLAPVQYFVATKLSQAQRSTLEYSNERLKQTNEMLRGIKLLKLYAWENIFRTRVETTRRKEMTSLRAFAIYTSISIFMNTAIPIAAVLITFVGHVSFFKEADFSPSVAFASLSLFHILVTPLFLLSSVVRSTVKALVSVQKLSEFLSSAEIREEQCAPHEPTPQGPASKYQAVPLRVVNRKRPAREDCRGLTGPLQSLVPSADGDADNCCVQIMGGYFTWTPDGIPTLSNITIRIPRGQLTMIVGQVGCGKSSLLLAALGEMQKVSGAVFWSSLPDSEIGEDPSPERETATDLDIRKRGPVAYASQKPWLLNATVEENIIFESPFNKQRYKMVIEACSLQPDIDILPHGDQTQIGERGINLSGGQRQRISVARALYQHANVVFLDDPFSALDIHLSDHLMQAGILELLRDDKRTVVLVTHKLQYLPHADWIIAMKDGTIQREGTLKDFQRSECQLFEHWKTLMNRQDQELEKETVTERKATEPPQGLSRAMSSRDGLLQDEEEEEEEAAESEEDDNLSSMLHQRAEIPWRACAKYLSSAGILLLSLLVFSQLLKHMVLVAIDYWLAKWTDSALTLTPAARNCSLSQECTLDQTVYAMVFTVLCSLGIVLCLVTSVTVEWTGLKVAKRLHRSLLNRIILAPMRFFETTPLGSILNRFSSDCNTIDQHIPSTLECLSRSTLLCVSALAVISYVTPVFLVALLPLAIVCYFIQKYFRVASRDLQQLDDTTQLPLLSHFAETVEGLTTIRAFRYEARFQQKLLEYTDSNNIASLFLTAANRWLEVRMEYIGACVVLIAAVTSISNSLHRELSAGLVGLGLTYALMVSNYLNWMVRNLADMELQLGAVKRIHGLLKTEAESYEGLLAPSLIPKNWPDQGKIQIQNLSVRYDSSLKPVLKHVNALIAPGQKIGICGRTGSGKSSFSLAFFRMVDTFEGHIIIDGIDIAKLPLHTLRSRLSIILQDPVLFSGTIRFNLDPERKCSDSTLWEALEIAQLKLVVKALPGGLDAIITEGGENFSQGQRQLFCLARAFVRKTSIFIMDEATASIDMATENILQKVVMTAFADRTVVTIAHRVHTILSADLVIVLKRGAILEFDKPEKLLSRKDSVFASFVRADK
  
Inhibitor
Name:
BDBM50118359
Synonyms:
(2-Chloro-7,7-dioxo-4,7-dihydro-1,7-dithia-4,6-diaza-inden-5-yl)-(1-methyl-cyclopropyl)-amine | (2-Chloro-7,7-dioxo-4,7-dihydro-1,7lambda*6*-dithia-4,6-diaza-inden-5-yl)-(1-methyl-cyclopropyl)-amine | 6-chloro-3-(1-methylcyclopropyl)-amino-4H-thieno[3,2-e]-1,2,4-thiadiazine1,1-dioxide | CHEMBL135191
Type:
Small organic molecule
Emp. Form.:
C9H10ClN3O2S2
Mol. Mass.:
291.778
SMILES:
CC1(CC1)NC1=Nc2cc(Cl)sc2S(=O)(=O)N1 |t:6|
Structure:
Search PDB for entries with ligand similarity: