Reaction Details |
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Target | Disintegrin and metalloproteinase domain-containing protein 17 |
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Ligand | BDBM50342970 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_744255 (CHEMBL1772062) |
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Ki | 7.6±n/a nM |
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Citation | Dai, C; Li, D; Popovici-Muller, J; Zhao, L; Girijavallabhan, VM; Rosner, KE; Lavey, BJ; Rizvi, R; Shankar, BB; Wong, MK; Guo, Z; Orth, P; Strickland, CO; Sun, J; Niu, X; Chen, S; Kozlowski, JA; Lundell, DJ; Piwinski, JJ; Shih, NY; Siddiqui, 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 |
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More Info.: | Get all data from this article, Assay Method |
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Disintegrin and metalloproteinase domain-containing protein 17 |
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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
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BDBM50342970 |
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n/a |
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Name | BDBM50342970 |
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 |
Type | Small organic molecule |
Emp. Form. | C25H27ClN4O5 |
Mol. Mass. | 498.959 |
SMILES | C[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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