| Reaction Details |
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 | Report a problem with these data |
| Target | Proto-oncogene tyrosine-protein kinase receptor Ret |
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| Ligand | BDBM50382959 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_818001 (CHEMBL2033427) |
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| Kd | 2±n/a nM |
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| Citation |  Rowbottom, MW; Faraoni, R; Chao, Q; Campbell, BT; Lai, AG; Setti, E; Ezawa, M; Sprankle, KG; Abraham, S; Tran, L; Struss, B; Gibney, M; Armstrong, RC; Gunawardane, RN; Nepomuceno, RR; Valenta, I; Hua, H; Gardner, MF; Cramer, MD; Gitnick, D; Insko, DE; Apuy, JL; Jones-Bolin, S; Ghose, AK; Herbertz, T; Ator, MA; Dorsey, BD; Ruggeri, B; Williams, M; Bhagwat, S; James, J; Holladay, MW Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E. J Med Chem55:1082-105 (2012) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Proto-oncogene tyrosine-protein kinase receptor Ret |
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| Name: | Proto-oncogene tyrosine-protein kinase receptor Ret |
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| Synonyms: | CDHF12 | CDHR16 | Cadherin family member 12 | PTC | Proto-oncogene c-Ret | RET | RET51 | RET_HUMAN | Tyrosine-protein kinase Ret (RET) |
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| Type: | Protein |
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| Mol. Mass.: | 124318.29 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P07949 |
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| Residue: | 1114 |
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| Sequence: | MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAP
EEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLT
VYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENR
PPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELV
AVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFD
ADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNR
NLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFA
QIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAE
LHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGR
CEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPR
GIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCY
HKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFP
RKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLK
QVNHPHVIKLYGACSQDGPLLLIVEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDH
PDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVY
EEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERL
FNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAA
STPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRA
DGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
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| BDBM50382959 |
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| n/a |
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| Name | BDBM50382959 |
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| Synonyms: | CEP-32496 | CHEMBL2029988 | US9730937, Example 261 |
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| Type | Small organic molecule |
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| Emp. Form. | C24H22F3N5O5 |
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| Mol. Mass. | 517.4572 |
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| SMILES | COc1cc2ncnc(Oc3cccc(NC(=O)Nc4cc(on4)C(C)(C)C(F)(F)F)c3)c2cc1OC |
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| Structure | 
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