Reaction Details |
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Target | Receptor tyrosine-protein kinase erbB-2 [1-775,'VC',777-1255] |
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Ligand | BDBM557881 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Cell Viability Assay and IC50 Estimation |
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IC50 | 520±n/a nM |
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Citation | Heymach, J; Robichaux, J; Nilsson, M; Jones, P; Cross, J; Theroff, J Heterocyclic inhibitors of tyrosine kinase US Patent US11365189 Publication Date 6/21/2022 |
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More Info.: | Get all data from this article, Assay Method |
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Receptor tyrosine-protein kinase erbB-2 [1-775,'VC',777-1255] |
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Name: | Receptor tyrosine-protein kinase erbB-2 [1-775,'VC',777-1255] |
Synonyms: | ERBB2 | ERBB2_HUMAN | HER2 | Her2 G776delinsVC(VC) | MLN19 | NEU | NGL |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 138039.69 |
Organism: | Homo sapiens (Human) |
Description: | P04626[1-775,'VC',777-1255] |
Residue: | 1256 |
Sequence: | MELAALCRWGLLLALLPPGAASTQVCTGTDMKLRLPASPETHLDMLRHLYQGCQVVQGNL
ELTYLPTNASLSFLQDIQEVQGYVLIAHNQVRQVPLQRLRIVRGTQLFEDNYALAVLDNG
DPLNNTTPVTGASPGGLRELQLRSLTEILKGGVLIQRNPQLCYQDTILWKDIFHKNNQLA
LTLIDTNRSRACHPCSPMCKGSRCWGESSEDCQSLTRTVCAGGCARCKGPLPTDCCHEQC
AAGCTGPKHSDCLACLHFNHSGICELHCPALVTYNTDTFESMPNPEGRYTFGASCVTACP
YNYLSTDVGSCTLVCPLHNQEVTAEDGTQRCEKCSKPCARVCYGLGMEHLREVRAVTSAN
IQEFAGCKKIFGSLAFLPESFDGDPASNTAPLQPEQLQVFETLEEITGYLYISAWPDSLP
DLSVFQNLQVIRGRILHNGAYSLTLQGLGISWLGLRSLRELGSGLALIHHNTHLCFVHTV
PWDQLFRNPHQALLHTANRPEDECVGEGLACHQLCARGHCWGPGPTQCVNCSQFLRGQEC
VEECRVLQGLPREYVNARHCLPCHPECQPQNGSVTCFGPEADQCVACAHYKDPPFCVARC
PSGVKPDLSYMPIWKFPDEEGACQPCPINCTHSCVDLDDKGCPAEQRASPLTSIISAVVG
ILLVVVLGVVFGILIKRRQQKIRKYTMRRLLQETELVEPLTPSGAMPNQAQMRILKETEL
RKVKVLGSGAFGTVYKGIWIPDGENVKIPVAIKVLRENTSPKANKEILDEAYVMAVCVGS
PYVSRLLGICLTSTVQLVTQLMPYGCLLDHVRENRGRLGSQDLLNWCMQIAKGMSYLEDV
RLVHRDLAARNVLVKSPNHVKITDFGLARLLDIDETEYHADGGKVPIKWMALESILRRRF
THQSDVWSYGVTVWELMTFGAKPYDGIPAREIPDLLEKGERLPQPPICTIDVYMIMVKCW
MIDSECRPRFRELVSEFSRMARDPQRFVVIQNEDLGPASPLDSTFYRSLLEDDDMGDLVD
AEEYLVPQQGFFCPDPAPGAGGMVHHRHRSSSTRSGGGDLTLGLEPSEEEAPRSPLAPSE
GAGSDVFDGDLGMGAAKGLQSLPTHDPSPLQRYSEDPTVPLPSETDGYVAPLTCSPQPEY
VNQPDVRPQPPSPREGPLPAARPAGATLERPKTLSPGKNGVVKDVFAFGGAVENPEYLTP
QGGAAPQPHPPPAFSPAFDNLYYWDQDPPERGAPPSTFKGTPTAENPEYLGLDVPV
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BDBM557881 |
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n/a |
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Name | BDBM557881 |
Synonyms: | 1-(3-((4-((4-bromo-3- chlorophenyl)amino)- pyrido[3,2-d]pyrimidin-6- yl)oxy)azetidin-1-yl)prop-2- en-1-one | US11365189, Ex. No. 99 |
Type | Small organic molecule |
Emp. Form. | C19H15BrClN5O2 |
Mol. Mass. | 460.712 |
SMILES | Clc1cc(Nc2ncnc3ccc(OC4CN(C4)C(=O)C=C)nc23)ccc1Br |
Structure |
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