Reaction Details |
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Target | A disintegrin and metalloproteinase with thrombospondin motifs 5 |
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Ligand | BDBM24065 |
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Substrate/Competitor | BDBM2 |
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Meas. Tech. | Kinesin ATPase In Vitro Assay |
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pH | 7±n/a |
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Temperature | 296.15±n/a K |
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IC50 | 24.7±7.5 nM |
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Citation | Cox, CD; Torrent, M; Breslin, MJ; Mariano, BJ; Whitman, DB; Coleman, PJ; Buser, CA; Walsh, ES; Hamilton, K; Schaber, MD; Lobell, RB; Tao, W; South, VJ; Kohl, NE; Yan, Y; Kuo, LC; Prueksaritanont, T; Slaughter, DE; Li, C; Mahan, E; Lu, B; Hartman, GD Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP. Bioorg Med Chem Lett16:3175-9 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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A disintegrin and metalloproteinase with thrombospondin motifs 5 |
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Name: | A disintegrin and metalloproteinase with thrombospondin motifs 5 |
Synonyms: | A disintegrin and metalloproteinase with thrombospondin motifs 5 (ADAMTS-5) | ADAMTS11 | ADAMTS5 | ADMP2 | ATS5_HUMAN | Aggrecanase-2 | Metalloproteinase with thrombospondin motifs 5 (ADAMTS-5) |
Type: | Enzyme |
Mol. Mass.: | 101769.09 |
Organism: | Homo sapiens (Human) |
Description: | Q9UNA0 |
Residue: | 930 |
Sequence: | MLLGWASLLLCAFRLPLAAVGPAATPAQDKAGQPPTAAAAAQPRRRQGEEVQERAEPPGH
PHPLAQRRRSKGLVQNIDQLYSGGGKVGYLVYAGGRRFLLDLERDGSVGIAGFVPAGGGT
SAPWRHRSHCFYRGTVDGSPRSLAVFDLCGGLDGFFAVKHARYTLKPLLRGPWAEEEKGR
VYGDGSARILHVYTREGFSFEALPPRASCETPASTPEAHEHAPAHSNPSGRAALASQLLD
QSALSPAGGSGPQTWWRRRRRSISRARQVELLLVADASMARLYGRGLQHYLLTLASIANR
LYSHASIENHIRLAVVKVVVLGDKDKSLEVSKNAATTLKNFCKWQHQHNQLGDDHEEHYD
AAILFTREDLCGHHSCDTLGMADVGTICSPERSCAVIEDDGLHAAFTVAHEIGHLLGLSH
DDSKFCEETFGSTEDKRLMSSILTSIDASKPWSKCTSATITEFLDDGHGNCLLDLPRKQI
LGPEELPGQTYDATQQCNLTFGPEYSVCPGMDVCARLWCAVVRQGQMVCLTKKLPAVEGT
PCGKGRICLQGKCVDKTKKKYYSTSSHGNWGSWGSWGQCSRSCGGGVQFAYRHCNNPAPR
NNGRYCTGKRAIYRSCSLMPCPPNGKSFRHEQCEAKNGYQSDAKGVKTFVEWVPKYAGVL
PADVCKLTCRAKGTGYYVVFSPKVTDGTECRLYSNSVCVRGKCVRTGCDGIIGSKLQYDK
CGVCGGDNSSCTKIVGTFNKKSKGYTDVVRIPEGATHIKVRQFKAKDQTRFTAYLALKKK
NGEYLINGKYMISTSETIIDINGTVMNYSGWSHRDDFLHGMGYSATKEILIVQILATDPT
KPLDVRYSFFVPKKSTPKVNSVTSHGSNKVGSHTSQPQWVTGPWLACSRTCDTGWHTRTV
QCQDGNRKLAKGCPLSQRPSAFKQCLLKKC
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BDBM24065 |
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BDBM2 |
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Name | BDBM24065 |
Synonyms: | 1-[(5S)-3-(2,5-difluorophenyl)-5-(3-hydroxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl]ethan-1-one | 3,5-diaryl-4,5-dihydropyrazole, 1 | CHEMBL195232 |
Type | Small organic molecule |
Emp. Form. | C17H14F2N2O2 |
Mol. Mass. | 316.3021 |
SMILES | CC(=O)N1N=C(C[C@H]1c1cccc(O)c1)c1cc(F)ccc1F |r,c:4| |
Structure |
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