Reaction Details |
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Target | Integrin alpha4beta7 |
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Ligand | BDBM16809 |
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Substrate/Competitor | MAdCAM-1 |
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Meas. Tech. | Ramos Cell Adhesion Assay (alpha4beta1 Mediated Adhesion/VCAM-1) |
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Temperature | 277.15±n/a K |
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IC50 | 2±n/a nM |
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Comments | extracted |
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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 Chem 49:3402-11 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Integrin alpha4beta7 |
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Name: | Integrin alpha4beta7 |
Synonyms: | n/a |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | The assay uses stably transfected K562 cells expressing human alpha4beta7 integrin. |
Components: | This complex has 2 components. |
Component 1 |
Name: | Integrin alpha4 |
Synonyms: | CD49d antigen | Integrin alpha-IV | VLA-4 |
Type: | Membrane Protein |
Mol. Mass.: | 115328.78 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 1038 |
Sequence: | MFPTESAWLGKRGANPGPEAAVRETVMLLLCLGVPTGRPYNVDTESALLYQGPHNTLFGY
SVVLHSHGANRWLLVGAPTANWLANASVINPGAIYRCRIGKNPGQTCEQLQLGSPNGEPC
GKTCLEERDNQWLGVTLSRQPGENGSIVTCGHRWKNIFYIKNENKLPTGGCYGVPPDLRT
ELSKRIAPCYQDYVKKFGENFASCQAGISSFYTKDLIVMGAPGSSYWTGSLFVYNITTNK
YKAFLDKQNQVKFGSYLGYSVGAGHFRSQHTTEVVGGAPQHEQIGKAYIFSIDEKELNIL
HEMKGKKLGSYFGASVCAVDLNADGFSDLLVGAPMQSTIREEGRVFVYINSGSGAVMNAM
ETNLVGSDKYAARFGESIVNLGDIDNDGFEDVAIGAPQEDDLQGAIYIYNGRADGISSTF
SQRIEGLQISKSLSMFGQSISGQIDADNNGYVDVAVGAFRSDSAVLLRTRPVVIVDASLS
HPESVNRTKFDCVENGWPSVCIDLTLCFSYKGKEVPGYIVLFYNMSLDVNRKAESPPRFY
FSSNGTSDVITGSIQVSSREANCRTHQAFMRKDVRDILTPIQIEAAYHLGPHVISKRSTE
EFPPLQPILQQKKEKDIMKKTINFARFCAHENCSADLQVSAKIGFLKPHENKTYLAVGSM
KTLMLNVSLFNAGDDAYETTLHVKLPVGLYFIKILELEEKQINCEVTDNSGVVQLDCSIG
YIYVDHLSRIDISFLLDVSSLSRAEEDLSITVHATCENEEEMDNLKHSRVTVAIPLKYEV
KLTVHGFVNPTSFVYGSNDENEPETCMVEKMNLTFHVINTGNSMAPNVSVEIMVPNSFSP
QTDKLFNILDVQTTTGECHFENYQRVCALEQQKSAMQTLKGIVRFLSKTDKRLLYCIKAD
PHCLNFLCNFGKMESGKEASVHIQLEGRPSILEMDETSALKFEIRATGFPEPNPRVIELN
KDENVAHVLLEGLHHQRPKRYFTIVIISSSLLLGLIVLLLISYVMWKAGFFKRQYKSILQ
EENRRDSWSYINSKSNDD
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Component 2 |
Name: | Integrin alpha-4/beta-7 |
Synonyms: | Integrin beta-7 precursor | Integrin beta7 |
Type: | Membrane Protein |
Mol. Mass.: | 86893.88 |
Organism: | Homo sapiens (Human) |
Description: | P26010 |
Residue: | 798 |
Sequence: | MVALPMVLVLLLVLSRGESELDAKIPSTGDATEWRNPHLSMLGSCQPAPSCQKCILSHPS
CAWCKQLNFTASGEAEARRCARREELLARGCPLEELEEPRGQQEVLQDQPLSQGARGEGA
TQLAPQRVRVTLRPGEPQQLQVRFLRAEGYPVDLYYLMDLSYSMKDDLERVRQLGHALLV
RLQEVTHSVRIGFGSFVDKTVLPFVSTVPSKLRHPCPTRLERCQSPFSFHHVLSLTGDAQ
AFEREVGRQSVSGNLDSPEGGFDAILQAALCQEQIGWRNVSRLLVFTSDDTFHTAGDGKL
GGIFMPSDGHCHLDSNGLYSRSTEFDYPSVGQVAQALSAANIQPIFAVTSAALPVYQELS
KLIPKSAVGELSEDSSNVVQLIMDAYNSLSSTVTLEHSSLPPGVHISYESQCEGPEKREG
KAEDRGQCNHVRINQTVTFWVSLQATHCLPEPHLLRLRALGFSEELIVELHTLCDCNCSD
TQPQAPHCSDGQGHLQCGVCSCAPGRLGRLCECSVAELSSPDLESGCRAPNGTGPLCSGK
GHCQCGRCSCSGQSSGHLCECDDASCERHEGILCGGFGRCQCGVCHCHANRTGRACECSG
DMDSCISPEGGLCSGHGRCKCNRCQCLDGYYGALCDQCPGCKTPCERHRDCAECGAFRTG
PLATNCSTACAHTNVTLALAPILDDGWCKERTLDNQLFFFLVEDDARGTVVLRVRPQEKG
ADHTQAIVLGCVGGIVAVGLGLVLAYRLSVEIYDRREYSRFEKEQQQLNWKQDSNPLYKS
AITTTINPRFQEADSPTL
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BDBM16809 |
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MAdCAM-1 |
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Name: | MAdCAM-1 |
Synonyms: | Mucosal addressin cell adhesion molecule 1 | hMAdCAM-1 |
Type: | Other Protein Type |
Mol. Mass.: | 42675.21 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant FLAG-hMAdCAM-1. |
Residue: | 406 |
Sequence: | MDFGLALLLAGLLGLLLGQSLQVKPLQVEPPEPVVAVALGASRQLTCRLACADRGASVQW
RGLDTSLGAVQSDTGRSVLTVRNASLSAAGTRVCVGSCGGRTFQHTVQLLVYAFPDQLTV
SPAALVPGDPEVACTAHKVTPVDPNALSFSLLVGGQELEGAQALGPEVQEEEEEPQGDED
VLFRVTERWRLPPLGTPVPPALYCQATMRLPGLELSHRQAIPVLHSPTSPEPPDTTSPEP
PNTTSPESPDTTSPESPDTTSQEPPDTTSQEPPDTTSQEPPDTTSPEPPDKTSPEPAPQQ
GSTHTPRSPGSTRTRRPEISQAGPTQGEVIPTGSSKPAGDQLPAALWTSSAVLGLLLLAL
PTYHLWKRCRHLAEDDTHPPASLRLLPQVSAWAGLRGTGQVGISPS
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