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TargetADAM17
LigandBDBM50342958
Substrate/Competitorn/a
Meas. Tech.ChEMBL_744255
Ki 1±n/a nM
Citation Dai CLi DPopovici-Muller JZhao LGirijavallabhan VMRosner KELavey BJRizvi RShankar BBWong MKGuo ZOrth PStrickland COSun JNiu XChen SKozlowski JALundell DJPiwinski JJShih NYSiddiqui MA 2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors. Bioorg Med Chem Lett 21:3172-6 (2011) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
ADAM17
Name:ADAM17
Synonyms:Disintegrin and metalloproteinase domain-containing protein 17 | Disintegrin and metalloproteinase domain-containing protein 17 (ADAM-17) | Disintegrin and metalloproteinase domain-containing protein 17 (ADAM17) | TACE | TNF-alpha convertase | TNF-alpha converting enzyme (TACE) | TNF-alpha-converting enzyme (TACE) | Tumor Necrosis Factor Alpha Converting Enzyme | Tumor necrosis factor-α converting enzyme (TACE)
Type:Enzyme
Mol. Mass.:93007.89
Organism:Homo sapiens (Human)
Description:
Residue:824
Sequence:
MRQSLLFLTSVVPFVLAPRPPDDPGFGPHQRLEKLDSLLSDYDILSLSNIQQHSVRKRDL
QTSTHVETLLTFSALKRHFKLYLTSSTERFSQNFKVVVVDGKNESEYTVKWQDFFTGHVV
GEPDSRVLAHIRDDDVIIRINTDGAEYNIEPLWRFVNDTKDKRMLVYKSEDIKNVSRLQS
PKVCGYLKVDNEELLPKGLVDREPPEELVHRVKRRADPDPMKNTCKLLVVADHRFYRYMG
RGEESTTTNYLIELIDRVDDIYRNTSWDNAGFKGYGIQIEQIRILKSPQEVKPGEKHYNM
AKSYPNEEKDAWDVKMLLEQFSFDIAEEASKVCLAHLFTYQDFDMGTLGLAYVGSPRANS
HGGVCPKAYYSPVGKKNIYLNSGLTSTKNYGKTILTKEADLVTTHELGHNFGAEHDPDGL
AECAPNEDQGGKYVMYPIAVSGDHENNKMFSNCSKQSIYKTIESKAQECFQERSNKVCGN
SRVDEGEECDPGIMYLNNDTCCNSDCTLKEGVQCSDRNSPCCKNCQFETAQKKCQEAINA
TCKGVSYCTGNSSECPPPGNAEDDTVCLDLGKCKDGKCIPFCEREQQLESCACNETDNSC
KVCCRDLSGRCVPYVDAEQKNLFLRKGKPCTVGFCDMNGKCEKRVQDVIERFWDFIDQLS
INTFGKFLADNIVGSVLVFSLIFWIPFSILVHCVDKKLDKQYESLSLFHPSNVEMLSSMD
SASVRIIKPFPAPQTPGRLQPAPVIPSAPAAPKLDHQRMDTIQEDPSTDSHMDEDGFEKD
PFPNSSTAAKSFEDLTDHPVTRSEKAASFKLQRQNRVDSKETEC
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50342958
n/a
NameBDBM50342958
Synonyms:(2R,3R)-N-((R)-1-(4-(1H-pyrazol-1-yl)phenyl)ethyl)-2,3-dihydroxy-4-((1R,3R,5R)-3-(2-(methylamino)thiazol-4-yl)-2-azabicyclo[3.1.0]hexan-2-yl)-4-oxobutanamide | CHEMBL1770824
TypeSmall organic molecule
Emp. Form.C24H28N6O4S
Mol. Mass.496.582
SMILESCNc1nc(cs1)[C@H]1C[C@H]2C[C@H]2N1C(=O)[C@H](O)[C@@H](O)C(=O)N[C@H](C)c1ccc(cc1)-n1cccn1 |r|
Structure
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