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TargetDisintegrin and metalloproteinase domain-containing protein 17
LigandBDBM50342970
Substrate/Competitorn/a
Meas. Tech.ChEMBL_744255 (CHEMBL1772062)
Ki 7.6±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 Lett21:3172-6 (2011) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Disintegrin and metalloproteinase domain-containing protein 17
Name:Disintegrin and metalloproteinase domain-containing protein 17
Synonyms:ADA17_HUMAN | ADAM17 | CSVP | 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:
BDBM50342970
n/a
NameBDBM50342970
Synonyms:CHEMBL1770633 | rac-(2R,3R)-N-((R)-1-(4-(1H-pyrazol-1-yl)phenyl)ethyl)-4-((4R)-2-(3-chlorophenyl)-4-hydroxypyrrolidin-1-yl)-2,3-dihydroxy-4-oxobutanamide
TypeSmall organic molecule
Emp. Form.C25H27ClN4O5
Mol. Mass.498.959
SMILESC[C@@H](NC(=O)[C@H](O)[C@@H](O)C(=O)N1C[C@H](O)CC1c1cccc(Cl)c1)c1ccc(cc1)-n1cccn1 |r|
Structure
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