Reaction Details |
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Target | Integrin alpha-4/beta-1 [T112H] |
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Ligand | BDBM16817 |
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Substrate/Competitor | VCAM-1 |
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Meas. Tech. | Ramos Cell Adhesion Assay (alpha4beta1 Mediated Adhesion/VCAM-1) |
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pH | 7.4±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 300±120 nM |
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Citation | Gong, Y; Barbay, JK; Dyatkin, AB; Miskowski, TA; Kimball, ES; Prouty, SM; Fisher, MC; Santulli, RJ; Schneider, CR; Wallace, NH; Ballentine, SA; Hageman, WE; Masucci, JA; Maryanoff, BE; Damiano, BP; Andrade-Gordon, P; Hlasta, DJ; Hornby, PJ; He, W Synthesis and biological evaluation of novel pyridazinone-based alpha4 integrin receptor antagonists. J Med Chem49:3402-11 (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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BDBM16817 |
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VCAM-1 |
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Name: | Vascular cell adhesion protein 1 |
Synonyms: | CD106 antigen | INCAM-100 | VCAM-1 | VCAM1 | VCAM1_HUMAN | Vascular cell adhesion protein 1 | Vascular cell adhesion protein 1 (VCAM-1) | Vascular cell adhesion protein 1 precursor |
Type: | Other Protein Type |
Mol. Mass.: | 81259.16 |
Organism: | Homo sapiens (Human) |
Description: | P19320 |
Residue: | 739 |
Sequence: | MPGKMVVILGASNILWIMFAASQAFKIETTPESRYLAQIGDSVSLTCSTTGCESPFFSWR
TQIDSPLNGKVTNEGTTSTLTMNPVSFGNEHSYLCTATCESRKLEKGIQVEIYSFPKDPE
IHLSGPLEAGKPITVKCSVADVYPFDRLEIDLLKGDHLMKSQEFLEDADRKSLETKSLEV
TFTPVIEDIGKVLVCRAKLHIDEMDSVPTVRQAVKELQVYISPKNTVISVNPSTKLQEGG
SVTMTCSSEGLPAPEIFWSKKLDNGNLQHLSGNATLTLIAMRMEDSGIYVCEGVNLIGKN
RKEVELIVQEKPFTVEISPGPRIAAQIGDSVMLTCSVMGCESPSFSWRTQIDSPLSGKVR
SEGTNSTLTLSPVSFENEHSYLCTVTCGHKKLEKGIQVELYSFPRDPEIEMSGGLVNGSS
VTVSCKVPSVYPLDRLEIELLKGETILENIEFLEDTDMKSLENKSLEMTFIPTIEDTGKA
LVCQAKLHIDDMEFEPKQRQSTQTLYVNVAPRDTTVLVSPSSILEEGSSVNMTCLSQGFP
APKILWSRQLPNGELQPLSENATLTLISTKMEDSGVYLCEGINQAGRSRKEVELIIQVTP
KDIKLTAFPSESVKEGDTVIISCTCGNVPETWIILKKKAETGDTVLKSIDGAYTIRKAQL
KDAGVYECESKNKVGSQLRSLTLDVQGRENNKDYFSPELLVLYFASSLIIPAIGMIIYFA
RKANMKGSYSLVEAQKSKV
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