| Reaction Details |
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 | Report a problem with these data |
| Target | Insulin-like growth factor 1 receptor |
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| Ligand | BDBM50299148 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_591853 (CHEMBL1045057) |
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| IC50 | 2±n/a nM |
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| Citation |  Wittman, MD; Carboni, JM; Yang, Z; Lee, FY; Antman, M; Attar, R; Balimane, P; Chang, C; Chen, C; Discenza, L; Frennesson, D; Gottardis, MM; Greer, A; Hurlburt, W; Johnson, W; Langley, DR; Li, A; Li, J; Liu, P; Mastalerz, H; Mathur, A; Menard, K; Patel, K; Sack, J; Sang, X; Saulnier, M; Smith, D; Stefanski, K; Trainor, G; Velaparthi, U; Zhang, G; Zimmermann, K; Vyas, DM Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development. J Med Chem52:7360-3 (2009) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Insulin-like growth factor 1 receptor |
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| Name: | Insulin-like growth factor 1 receptor |
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| Synonyms: | CD_antigen=CD221 | IGF-I receptor | IGF1R | IGF1R_HUMAN | Insulin-like growth factor 1 receptor (IGF1R) | Insulin-like growth factor 1 receptor (IGFIR) | Insulin-like growth factor 1 receptor alpha chain | Insulin-like growth factor 1 receptor beta chain | Insulin-like growth factor I receptor | Insulin-like growth factor receptor (IGFR) |
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| Type: | Protein |
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| Mol. Mass.: | 154776.79 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P08069 |
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| Residue: | 1367 |
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| Sequence: | MKSGSGGGSPTSLWGLLFLSAALSLWPTSGEICGPGIDIRNDYQQLKRLENCTVIEGYLH
ILLISKAEDYRSYRFPKLTVITEYLLLFRVAGLESLGDLFPNLTVIRGWKLFYNYALVIF
EMTNLKDIGLYNLRNITRGAIRIEKNADLCYLSTVDWSLILDAVSNNYIVGNKPPKECGD
LCPGTMEEKPMCEKTTINNEYNYRCWTTNRCQKMCPSTCGKRACTENNECCHPECLGSCS
APDNDTACVACRHYYYAGVCVPACPPNTYRFEGWRCVDRDFCANILSAESSDSEGFVIHD
GECMQECPSGFIRNGSQSMYCIPCEGPCPKVCEEEKKTKTIDSVTSAQMLQGCTIFKGNL
LINIRRGNNIASELENFMGLIEVVTGYVKIRHSHALVSLSFLKNLRLILGEEQLEGNYSF
YVLDNQNLQQLWDWDHRNLTIKAGKMYFAFNPKLCVSEIYRMEEVTGTKGRQSKGDINTR
NNGERASCESDVLHFTSTTTSKNRIIITWHRYRPPDYRDLISFTVYYKEAPFKNVTEYDG
QDACGSNSWNMVDVDLPPNKDVEPGILLHGLKPWTQYAVYVKAVTLTMVENDHIRGAKSE
ILYIRTNASVPSIPLDVLSASNSSSQLIVKWNPPSLPNGNLSYYIVRWQRQPQDGYLYRH
NYCSKDKIPIRKYADGTIDIEEVTENPKTEVCGGEKGPCCACPKTEAEKQAEKEEAEYRK
VFENFLHNSIFVPRPERKRRDVMQVANTTMSSRSRNTTAADTYNITDPEELETEYPFFES
RVDNKERTVISNLRPFTLYRIDIHSCNHEAEKLGCSASNFVFARTMPAEGADDIPGPVTW
EPRPENSIFLKWPEPENPNGLILMYEIKYGSQVEDQRECVSRQEYRKYGGAKLNRLNPGN
YTARIQATSLSGNGSWTDPVFFYVQAKTGYENFIHLIIALPVAVLLIVGGLVIMLYVFHR
KRNNSRLGNGVLYASVNPEYFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKG
VVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIME
LMTRGDLKSYLRSLRPEMENNPVLAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARN
CMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGV
VLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFL
EIISSIKEEMEPGFREVSFYYSEENKLPEPEELDLEPENMESVPLDPSASSSSLPLPDRH
SGHKAENGPGPGVLVLRASFDERQPYAHMNGGRKNERALPLPQSSTC
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| BDBM50299148 |
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| n/a |
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| Name | BDBM50299148 |
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| Synonyms: | (S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide | 1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl}-N-(6-fluoropyridin-3-yl)-2-methyl-L-prolinamide | BMS-754807 | CHEMBL575448 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H24FN9O |
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| Mol. Mass. | 461.4948 |
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| SMILES | C[C@]1(CCCN1c1nc(Nc2cc([nH]n2)C2CC2)c2cccn2n1)C(=O)Nc1ccc(F)nc1 |r| |
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| Structure | 
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