| Reaction Details |
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 | Report a problem with these data |
| Target | Kinesin-1 heavy chain/Proto-oncogene tyrosine-protein kinase receptor Ret |
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| Ligand | BDBM50538514 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1972971 (CHEMBL4605789) |
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| IC50 | 1.7±n/a nM |
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| Citation |  Mathison, CJN; Chianelli, D; Rucker, PV; Nelson, J; Roland, J; Huang, Z; Yang, Y; Jiang, J; Xie, YF; Epple, R; Bursulaya, B; Lee, C; Gao, MY; Shaffer, J; Briones, S; Sarkisova, Y; Galkin, A; Li, L; Li, N; Li, C; Hua, S; Kasibhatla, S; Kinyamu-Akunda, J; Kikkawa, R; Molteni, V; Tellew, JE Efficacy and Tolerability of Pyrazolo[1,5- ACS Med Chem Lett11:558-565 (2020) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Kinesin-1 heavy chain/Proto-oncogene tyrosine-protein kinase receptor Ret |
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| Name: | Kinesin-1 heavy chain/Proto-oncogene tyrosine-protein kinase receptor Ret |
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| Synonyms: | Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET |
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| Type: | n/a |
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| Mol. Mass.: | n/a |
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| Description: | ASSAY_ID of ChEMBL is 1972971 |
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| Components: | This complex has 2 components. |
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| Component 1 |
| 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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| Component 2 |
| Name: | Kinesin-1 heavy chain |
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| Synonyms: | KIF5B | KINH_HUMAN | KNS | KNS1 |
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| Type: | PROTEIN |
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| Mol. Mass.: | 109682.61 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_770435 |
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| Residue: | 963 |
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| Sequence: | MADLAECNIKVMCRFRPLNESEVNRGDKYIAKFQGEDTVVIASKPYAFDRVFQSSTSQEQ
VYNDCAKKIVKDVLEGYNGTIFAYGQTSSGKTHTMEGKLHDPEGMGIIPRIVQDIFNYIY
SMDENLEFHIKVSYFEIYLDKIRDLLDVSKTNLSVHEDKNRVPYVKGCTERFVCSPDEVM
DTIDEGKSNRHVAVTNMNEHSSRSHSIFLINVKQENTQTEQKLSGKLYLVDLAGSEKVSK
TGAEGAVLDEAKNINKSLSALGNVISALAEGSTYVPYRDSKMTRILQDSLGGNCRTTIVI
CCSPSSYNESETKSTLLFGQRAKTIKNTVCVNVELTAEQWKKKYEKEKEKNKILRNTIQW
LENELNRWRNGETVPIDEQFDKEKANLEAFTVDKDITLTNDKPATAIGVIGNFTDAERRK
CEEEIAKLYKQLDDKDEEINQQSQLVEKLKTQMLDQEELLASTRRDQDNMQAELNRLQAE
NDASKEEVKEVLQALEELAVNYDQKSQEVEDKTKEYELLSDELNQKSATLASIDAELQKL
KEMTNHQKKRAAEMMASLLKDLAEIGIAVGNNDVKQPEGTGMIDEEFTVARLYISKMKSE
VKTMVKRCKQLESTQTESNKKMEENEKELAACQLRISQHEAKIKSLTEYLQNVEQKKRQL
EESVDALSEELVQLRAQEKVHEMEKEHLNKVQTANEVKQAVEQQIQSHRETHQKQISSLR
DEVEAKAKLITDLQDQNQKMMLEQERLRVEHEKLKATDQEKSRKLHELTVMQDRREQARQ
DLKGLEETVAKELQTLHNLRKLFVQDLATRVKKSAEIDSDDTGGSAAQKQKISFLENNLE
QLTKVHKQLVRDNADLRCELPKLEKRLRATAERVKALESALKEAKENASRDRKRYQQEVD
RIKEAVRSKNMARRGHSAQIAKPIRPGQHPAASPTHPSAIRGGGAFVQNSQPVAVRGGGG
KQV
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| BDBM50538514 |
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| n/a |
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| Name | BDBM50538514 |
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| Synonyms: | CHEMBL4644274 |
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| Type | Small organic molecule |
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| Emp. Form. | C30H38N6O2 |
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| Mol. Mass. | 514.6617 |
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| SMILES | COc1ccc(cc1OC)-c1cnn2c(N)c(c(NC3CC(C)(C)N(C)C(C)(C)C3)nc12)-c1ccccc1 |
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| Structure | 
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