Reaction Details |
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Target | Integrin alpha-4/beta-1 [T112H] |
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Ligand | BDBM17931 |
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Substrate/Competitor | Eu-Labeled Human VCAM-1/Fc Chimera |
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Meas. Tech. | VLA-4/VCAM-1 binding assay |
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pH | 7.5±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 1.0±n/a nM |
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Citation | Chiba, J; Takayama, G; Takashi, T; Yokoyama, M; Nakayama, A; Baldwin, JJ; McDonald, E; Moriarty, KJ; Sarko, CR; Saionz, KW; Swanson, R; Hussain, Z; Wong, A; Machinaga, N Synthesis, biological evaluation, and pharmacokinetic study of prolyl-1-piperazinylacetic acid and prolyl-4-piperidinylacetic acid derivatives as VLA-4 antagonists. Bioorg Med Chem14:2725-46 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Integrin alpha-4/beta-1 [T112H] |
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Name: | Integrin alpha-4/beta-1 [T112H] |
Synonyms: | CD49d/CD29 | Integrin alpha4beta1 (VLA-4) | Very Late Antigen-4 |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | The assay uses transfected Ramos cells expressing alpha4beta1 integrin. |
Components: | This complex has 2 components. |
Component 1 |
Name: | Integrin alpha-4 |
Synonyms: | CD49 antigen-like family member D | CD49D | CD49d antigen | CD_antigen=CD49d | ITA4_HUMAN | ITGA4 | Integrin alpha-4 | Integrin alpha-4/beta-7 | Integrin alpha-IV | Integrin alpha4 | VLA-4 | VLA-4 subunit alpha | integrin alpha 4 precursor | integrin alpha-4 precursor |
Type: | Membrane Protein |
Mol. Mass.: | 114897.35 |
Organism: | Homo sapiens (Human) |
Description: | P13612 |
Residue: | 1032 |
Sequence: | MAWEARREPGPRRAAVRETVMLLLCLGVPTGRPYNVDTESALLYQGPHNTLFGYSVVLHS
HGANRWLLVGAPTANWLANASVINPGAIYRCRIGKNPGQTCEQLQLGSPNGEPCGKTCLE
ERDNQWLGVTLSRQPGENGSIVTCGHRWKNIFYIKNENKLPTGGCYGVPPDLRTELSKRI
APCYQDYVKKFGENFASCQAGISSFYTKDLIVMGAPGSSYWTGSLFVYNITTNKYKAFLD
KQNQVKFGSYLGYSVGAGHFRSQHTTEVVGGAPQHEQIGKAYIFSIDEKELNILHEMKGK
KLGSYFGASVCAVDLNADGFSDLLVGAPMQSTIREEGRVFVYINSGSGAVMNAMETNLVG
SDKYAARFGESIVNLGDIDNDGFEDVAIGAPQEDDLQGAIYIYNGRADGISSTFSQRIEG
LQISKSLSMFGQSISGQIDADNNGYVDVAVGAFRSDSAVLLRTRPVVIVDASLSHPESVN
RTKFDCVENGWPSVCIDLTLCFSYKGKEVPGYIVLFYNMSLDVNRKAESPPRFYFSSNGT
SDVITGSIQVSSREANCRTHQAFMRKDVRDILTPIQIEAAYHLGPHVISKRSTEEFPPLQ
PILQQKKEKDIMKKTINFARFCAHENCSADLQVSAKIGFLKPHENKTYLAVGSMKTLMLN
VSLFNAGDDAYETTLHVKLPVGLYFIKILELEEKQINCEVTDNSGVVQLDCSIGYIYVDH
LSRIDISFLLDVSSLSRAEEDLSITVHATCENEEEMDNLKHSRVTVAIPLKYEVKLTVHG
FVNPTSFVYGSNDENEPETCMVEKMNLTFHVINTGNSMAPNVSVEIMVPNSFSPQTDKLF
NILDVQTTTGECHFENYQRVCALEQQKSAMQTLKGIVRFLSKTDKRLLYCIKADPHCLNF
LCNFGKMESGKEASVHIQLEGRPSILEMDETSALKFEIRATGFPEPNPRVIELNKDENVA
HVLLEGLHHQRPKRYFTIVIISSSLLLGLIVLLLISYVMWKAGFFKRQYKSILQEENRRD
SWSYINSKSNDD
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Component 2 |
Name: | Integrin beta-1 [T112H] |
Synonyms: | CD29 antigen | FNRB | Fibronectin receptor subunit beta | ITB1_HUMAN | ITGB1 | Integrin VLA-4 subunit beta | Integrin beta1 | MDF2 | MSK12 |
Type: | Membrane Protein |
Mol. Mass.: | 88450.95 |
Organism: | Homo sapiens (Human) |
Description: | P05556[T112H] |
Residue: | 798 |
Sequence: | MNLQPIFWIGLISSVCCVFAQTDENRCLKANAKSCGECIQAGPNCGWCTNSTFLQEGMPT
SARCDDLEALKKKGCPPDDIENPRGSKDIKKNKNVTNRSKGTAEKLKPEDIHQIQPQQLV
LRLRSGEPQTFTLKFKRAEDYPIDLYYLMDLSYSMKDDLENVKSLGTDLMNEMRRITSDF
RIGFGSFVEKTVMPYISTTPAKLRNPCTSEQNCTTPFSYKNVLSLTNKGEVFNELVGKQR
ISGNLDSPEGGFDAIMQVAVCGSLIGWRNVTRLLVFSTDAGFHFAGDGKLGGIVLPNDGQ
CHLENNMYTMSHYYDYPSIAHLVQKLSENNIQTIFAVTEEFQPVYKELKNLIPKSAVGTL
SANSSNVIQLIIDAYNSLSSEVILENGKLSEGVTISYKSYCKNGVNGTGENGRKCSNISI
GDEVQFEISITSNKCPKKDSDSFKIRPLGFTEEVEVILQYICECECQSEGIPESPKCHEG
NGTFECGACRCNEGRVGRHCECSTDEVNSEDMDAYCRKENSSEICSNNGECVCGQCVCRK
RDNTNEIYSGKFCECDNFNCDRSNGLICGGNGVCKCRVCECNPNYTGSACDCSLDTSTCE
ASNGQICNGRGICECGVCKCTDPKFQGQTCEMCQTCLGVCAEHKECVQCRAFNKGEKKDT
CTQECSYFNITKVESRDKLPQPVQPDPVSHCKEKDVDDCWFYFTYSVNGNNEVMVHVVEN
PECPTGPDIIPIVAGVVAGIVLIGLALLLIWKLLMIIHDRREFAKFEKEKMNAKWDTGEN
PIYKSAVTTVVNPKYEGK
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BDBM17931 |
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Eu-Labeled Human VCAM-1/Fc Chimera |
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Name: | Eu-Labeled Human VCAM-1/Fc Chimera |
Synonyms: | Recombinant Human VCAM-1/CD106/Fc Chimera |
Type: | Other Protein Type |
Mol. Mass.: | 358.43 |
Organism: | n/a |
Description: | A DNA sequence encoding the signal peptide from human CD33 joined with amino acid residues 25-698 of the extracellular domain of human vascular cell adhesion molecule 1 was fused to the 6X histidine tagged Fc of human IgG1 via a polypeptide linker. The chimeric protein was expressed in a mouse myeloma cell line, NS0. |
Residue: | 3 |
Sequence: | |