Reaction Details |
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Target | High affinity nerve growth factor receptor |
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Ligand | BDBM136597 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2250561 (CHEMBL5164771) |
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IC50 | 272±n/a nM |
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Citation | Wang, Z; Wang, J; Wang, Y; Xiang, S; Song, X; Tu, Z; Zhou, Y; Zhang, ZM; Zhang, Z; Ding, K; Lu, X Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance. J Med Chem65:6325-6337 (2022) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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High affinity nerve growth factor receptor |
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Name: | High affinity nerve growth factor receptor |
Synonyms: | 2.7.10.1 | MTC | NTRK1 | NTRK1/NTRK2 | NTRK1_HUMAN | Nerve growth factor receptor Trk-A | Neurotrophic tyrosine kinase receptor type 1 | Neurotrophic tyrosine kinase receptor type 1 (TrkA) | Synonyms=MTC | TRK | TRK1-transforming tyrosine kinase protein | TRKA | TRKA GN | TRKA GN | Trk-A | Tropomyosin alpha-3 chain/High affinity nerve growth factor receptor | Tropomyosin-related kinase A | Tropomyosin-related kinase A (TrkA) | Tyrosine kinase receptor | Tyrosine kinase receptor (Trk) | Tyrosine kinase receptor A | Tyrosine kinase receptor A (Trk A) | Tyrosine kinase receptor A (Trk-A) | Tyrosine kinase receptor A (TrkA) | gp140trk | p140-TrkA |
Type: | n/a |
Mol. Mass.: | 87498.18 |
Organism: | Homo sapiens (Human) |
Description: | P04629 |
Residue: | 796 |
Sequence: | MLRGGRRGQLGWHSWAAGPGSLLAWLILASAGAAPCPDACCPHGSSGLRCTRDGALDSLH
HLPGAENLTELYIENQQHLQHLELRDLRGLGELRNLTIVKSGLRFVAPDAFHFTPRLSRL
NLSFNALESLSWKTVQGLSLQELVLSGNPLHCSCALRWLQRWEEEGLGGVPEQKLQCHGQ
GPLAHMPNASCGVPTLKVQVPNASVDVGDDVLLRCQVEGRGLEQAGWILTELEQSATVMK
SGGLPSLGLTLANVTSDLNRKNVTCWAENDVGRAEVSVQVNVSFPASVQLHTAVEMHHWC
IPFSVDGQPAPSLRWLFNGSVLNETSFIFTEFLEPAANETVRHGCLRLNQPTHVNNGNYT
LLAANPFGQASASIMAAFMDNPFEFNPEDPIPVSFSPVDTNSTSGDPVEKKDETPFGVSV
AVGLAVFACLFLSTLLLVLNKCGRRNKFGINRPAVLAPEDGLAMSLHFMTLGGSSLSPTE
GKGSGLQGHIIENPQYFSDACVHHIKRRDIVLKWELGEGAFGKVFLAECHNLLPEQDKML
VAVKALKEASESARQDFQREAELLTMLQHQHIVRFFGVCTEGRPLLMVFEYMRHGDLNRF
LRSHGPDAKLLAGGEDVAPGPLGLGQLLAVASQVAAGMVYLAGLHFVHRDLATRNCLVGQ
GLVVKIGDFGMSRDIYSTDYYRVGGRTMLPIRWMPPESILYRKFTTESDVWSFGVVLWEI
FTYGKQPWYQLSNTEAIDCITQGRELERPRACPPEVYAIMRGCWQREPQQRHSIKDVHAR
LQALAQAPPVYLDVLG
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BDBM136597 |
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n/a |
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Name | BDBM136597 |
Synonyms: | US10005783, 14 | US10047097, 14 | US10774085, Example 14 | US11098046, Compound LOXO-101 | US11267818, Example 14 | US11453672, Example L-7 | US8865698, 14 | US9676783, 14 |
Type | Small organic molecule |
Emp. Form. | C21H22F2N6O2 |
Mol. Mass. | 428.4352 |
SMILES | O[C@H]1CCN(C1)C(=O)Nc1cnn2ccc(nc12)N1CCC[C@@H]1c1cc(F)ccc1F |r| |
Structure |
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