Reaction Details |
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Target | Receptor tyrosine-protein kinase erbB-4 |
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Ligand | BDBM50256480 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_519644 (CHEMBL946771) |
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IC50 | >25000±n/a nM |
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Citation | Emmitte, KA; Wilson, BJ; Baum, EW; Emerson, HK; Kuntz, KW; Nailor, KE; Salovich, JM; Smith, SC; Cheung, M; Gerding, RM; Stevens, KL; Uehling, DE; Mook, RA; Moorthy, GS; Dickerson, SH; Hassell, AM; Leesnitzer, MA; Shewchuk, LM; Groy, A; Rowand, JL; Anderson, K; Atkins, CL; Yang, J; Sabbatini, P; Kumar, R Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R). Bioorg Med Chem Lett19:1004-8 (2009) [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-4 |
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Name: | Receptor tyrosine-protein kinase erbB-4 |
Synonyms: | ERBB4 | ERBB4_HUMAN | Epidermal growth factor receptor | Epidermal growth factor receptor 4 (ERBB4) | ErbB-4 (HER4) Tyrosine Kinase | HER4 | Proto-oncogene c-ErbB-4 | Proto-oncogene-like protein c-ErbB-4 | Receptor protein-tyrosine kinase erbB-4 | Tyrosine kinase-type cell surface receptor HER4 | Tyrosine kinase-type cell surface receptor HER4 (HER4) |
Type: | Protein |
Mol. Mass.: | 146803.56 |
Organism: | Homo sapiens (Human) |
Description: | Q15303 |
Residue: | 1308 |
Sequence: | MKPATGLWVWVSLLVAAGTVQPSDSQSVCAGTENKLSSLSDLEQQYRALRKYYENCEVVM
GNLEITSIEHNRDLSFLRSVREVTGYVLVALNQFRYLPLENLRIIRGTKLYEDRYALAIF
LNYRKDGNFGLQELGLKNLTEILNGGVYVDQNKFLCYADTIHWQDIVRNPWPSNLTLVST
NGSSGCGRCHKSCTGRCWGPTENHCQTLTRTVCAEQCDGRCYGPYVSDCCHRECAGGCSG
PKDTDCFACMNFNDSGACVTQCPQTFVYNPTTFQLEHNFNAKYTYGAFCVKKCPHNFVVD
SSSCVRACPSSKMEVEENGIKMCKPCTDICPKACDGIGTGSLMSAQTVDSSNIDKFINCT
KINGNLIFLVTGIHGDPYNAIEAIDPEKLNVFRTVREITGFLNIQSWPPNMTDFSVFSNL
VTIGGRVLYSGLSLLILKQQGITSLQFQSLKEISAGNIYITDNSNLCYYHTINWTTLFST
INQRIVIRDNRKAENCTAEGMVCNHLCSSDGCWGPGPDQCLSCRRFSRGRICIESCNLYD
GEFREFENGSICVECDPQCEKMEDGLLTCHGPGPDNCTKCSHFKDGPNCVEKCPDGLQGA
NSFIFKYADPDRECHPCHPNCTQGCNGPTSHDCIYYPWTGHSTLPQHARTPLIAAGVIGG
LFILVIVGLTFAVYVRRKSIKKKRALRRFLETELVEPLTPSGTAPNQAQLRILKETELKR
VKVLGSGAFGTVYKGIWVPEGETVKIPVAIKILNETTGPKANVEFMDEALIMASMDHPHL
VRLLGVCLSPTIQLVTQLMPHGCLLEYVHEHKDNIGSQLLLNWCVQIAKGMMYLEERRLV
HRDLAARNVLVKSPNHVKITDFGLARLLEGDEKEYNADGGKMPIKWMALECIHYRKFTHQ
SDVWSYGVTIWELMTFGGKPYDGIPTREIPDLLEKGERLPQPPICTIDVYMVMVKCWMID
ADSRPKFKELAAEFSRMARDPQRYLVIQGDDRMKLPSPNDSKFFQNLLDEEDLEDMMDAE
EYLVPQAFNIPPPIYTSRARIDSNRSEIGHSPPPAYTPMSGNQFVYRDGGFAAEQGVSVP
YRAPTSTIPEAPVAQGATAEIFDDSCCNGTLRKPVAPHVQEDSSTQRYSADPTVFAPERS
PRGELDEEGYMTPMRDKPKQEYLNPVEENPFVSRRKNGDLQALDNPEYHNASNGPPKAED
EYVNEPLYLNTFANTLGKAEYLKNNILSMPEKAKKAFDNPDYWNHSLPPRSTLQHPDYLQ
EYSTKYFYKQNGRIRPIVAENPEYLSEFSLKPGTVLPPPPYRHRNTVV
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BDBM50256480 |
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n/a |
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Name | BDBM50256480 |
Synonyms: | CHEMBL466397 | N-(2,6-difluorophenyl)-5-(3-(2-(5-ethyl-2-methoxy-4-(4-(4-(methylsulfonyl)piperazin-1-yl)piperidin-1-yl)phenylamino)pyrimidin-4-yl)imidazo[1,2-a]pyridin-2-yl)-2-methoxybenzamide |
Type | Small organic molecule |
Emp. Form. | C44H47F2N9O5S |
Mol. Mass. | 851.963 |
SMILES | CCc1cc(Nc2nccc(n2)-c2c(nc3ccccn23)-c2ccc(OC)c(c2)C(=O)Nc2c(F)cccc2F)c(OC)cc1N1CCC(CC1)N1CCN(CC1)S(C)(=O)=O |
Structure |
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