| Reaction Details |
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 | Report a problem with these data |
| Target | Receptor tyrosine-protein kinase erbB-3 |
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| Ligand | BDBM50112173 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1743852 (CHEMBL4178362) |
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| IC50 | 2.0±n/a nM |
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| Citation |  Planken, S; Behenna, DC; Nair, SK; Johnson, TO; Nagata, A; Almaden, C; Bailey, S; Ballard, TE; Bernier, L; Cheng, H; Cho-Schultz, S; Dalvie, D; Deal, JG; Dinh, DM; Edwards, MP; Ferre, RA; Gajiwala, KS; Hemkens, M; Kania, RS; Kath, JC; Matthews, J; Murray, BW; Niessen, S; Orr, ST; Pairish, M; Sach, NW; Shen, H; Shi, M; Solowiej, J; Tran, K; Tseng, E; Vicini, P; Wang, Y; Weinrich, SL; Zhou, R; Zientek, M; Liu, L; Luo, Y; Xin, S; Zhang, C; Lafontaine, J Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR. J Med Chem60:3002-3019 (2017) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Receptor tyrosine-protein kinase erbB-3 |
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| Name: | Receptor tyrosine-protein kinase erbB-3 |
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| Synonyms: | ERBB3 | ERBB3_HUMAN | HER3 | Proto-oncogene-like protein c-ErbB-3 | Tyrosine kinase-type cell surface receptor HER3 |
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| Type: | PROTEIN |
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| Mol. Mass.: | 148097.73 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_774331 |
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| Residue: | 1342 |
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| Sequence: | MRANDALQVLGLLFSLARGSEVGNSQAVCPGTLNGLSVTGDAENQYQTLYKLYERCEVVM
GNLEIVLTGHNADLSFLQWIREVTGYVLVAMNEFSTLPLPNLRVVRGTQVYDGKFAIFVM
LNYNTNSSHALRQLRLTQLTEILSGGVYIEKNDKLCHMDTIDWRDIVRDRDAEIVVKDNG
RSCPPCHEVCKGRCWGPGSEDCQTLTKTICAPQCNGHCFGPNPNQCCHDECAGGCSGPQD
TDCFACRHFNDSGACVPRCPQPLVYNKLTFQLEPNPHTKYQYGGVCVASCPHNFVVDQTS
CVRACPPDKMEVDKNGLKMCEPCGGLCPKACEGTGSGSRFQTVDSSNIDGFVNCTKILGN
LDFLITGLNGDPWHKIPALDPEKLNVFRTVREITGYLNIQSWPPHMHNFSVFSNLTTIGG
RSLYNRGFSLLIMKNLNVTSLGFRSLKEISAGRIYISANRQLCYHHSLNWTKVLRGPTEE
RLDIKHNRPRRDCVAEGKVCDPLCSSGGCWGPGPGQCLSCRNYSRGGVCVTHCNFLNGEP
REFAHEAECFSCHPECQPMEGTATCNGSGSDTCAQCAHFRDGPHCVSSCPHGVLGAKGPI
YKYPDVQNECRPCHENCTQGCKGPELQDCLGQTLVLIGKTHLTMALTVIAGLVVIFMMLG
GTFLYWRGRRIQNKRAMRRYLERGESIEPLDPSEKANKVLARIFKETELRKLKVLGSGVF
GTVHKGVWIPEGESIKIPVCIKVIEDKSGRQSFQAVTDHMLAIGSLDHAHIVRLLGLCPG
SSLQLVTQYLPLGSLLDHVRQHRGALGPQLLLNWGVQIAKGMYYLEEHGMVHRNLAARNV
LLKSPSQVQVADFGVADLLPPDDKQLLYSEAKTPIKWMALESIHFGKYTHQSDVWSYGVT
VWELMTFGAEPYAGLRLAEVPDLLEKGERLAQPQICTIDVYMVMVKCWMIDENIRPTFKE
LANEFTRMARDPPRYLVIKRESGPGIAPGPEPHGLTNKKLEEVELEPELDLDLDLEAEED
NLATTTLGSALSLPVGTLNRPRGSQSLLSPSSGYMPMNQGNLGESCQESAVSGSSERCPR
PVSLHPMPRGCLASESSEGHVTGSEAELQEKVSMCRSRSRSRSPRPRGDSAYHSQRHSLL
TPVTPLSPPGLEEEDVNGYVMPDTHLKGTPSSREGTLSSVGLSSVLGTEEEDEDEEYEYM
NRRRRHSPPHPPRPSSLEELGYEYMDVGSDLSASLGSTQSCPLHPVPIMPTAGTTPDEDY
EYMNRQRDGGGPGGDYAAMGACPASEQGYEEMRAFQGPGHQAPHVHYARLKTLRSLEATD
SAFDNPDYWHSRLFPKANAQRT
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| BDBM50112173 |
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| n/a |
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| Name | BDBM50112173 |
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| Synonyms: | CHEMBL3608429 |
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| Type | Small organic molecule |
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| Emp. Form. | C19H24FN9O |
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| Mol. Mass. | 413.452 |
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| SMILES | CC(C)n1cnc2c(Nc3cnn(C)c3)nc(nc12)N1C[C@@H](F)[C@@H](C1)NC(=O)C=C |r| |
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| Structure | 
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