Reaction Details |
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Target | Cell division cycle 7-related protein kinase/Protein DBF4 homolog A |
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Ligand | BDBM158154 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1577171 (CHEMBL3807433) |
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IC50 | >10000±n/a nM |
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Citation | Menichincheri, M; Ardini, E; Magnaghi, P; Avanzi, N; Banfi, P; Bossi, R; Buffa, L; Canevari, G; Ceriani, L; Colombo, M; Corti, L; Donati, D; Fasolini, M; Felder, E; Fiorelli, C; Fiorentini, F; Galvani, A; Isacchi, A; Borgia, AL; Marchionni, C; Nesi, M; Orrenius, C; Panzeri, A; Pesenti, E; Rusconi, L; Saccardo, MB; Vanotti, E; Perrone, E; Orsini, P Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor. J Med Chem59:3392-408 (2016) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Cell division cycle 7-related protein kinase/Protein DBF4 homolog A |
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Name: | Cell division cycle 7-related protein kinase/Protein DBF4 homolog A |
Synonyms: | Activator of S phase kinase DBF4/Cell division cycle 7-related protein kinase | CDC7 and DBF4 | CDC7/DBF4 (Cell division cycle 7-related protein kinase/Activator of S phase kinase) |
Type: | Protein |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
Name: | Protein DBF4 homolog A |
Synonyms: | ASK | Activator of S phase kinase | Chiffon homolog A | DBF4 | DBF4-type zinc finger-containing protein 1 | DBF4A | DBF4A_HUMAN | Protein DBF4 homolog A | ZDBF1 |
Type: | Regulatory subunit |
Mol. Mass.: | 76869.65 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 674 |
Sequence: | MNSGAMRIHSKGHFQGGIQVKNEKNRPSLKSLKTDNRPEKSKCKPLWGKVFYLDLPSVTI
SEKLQKDIKDLGGRVEEFLSKDISYLISNKKEAKFAQTLGRISPVPSPESAYTAETTSPH
PSHDGSSFKSPDTVCLSRGKLLVEKAIKDHDFIPSNSILSNALSWGVKILHIDDIRYYIE
QKKKELYLLKKSSTSVRDGGKRVGSGAQKTRTGRLKKPFVKVEDMSQLYRPFYLQLTNMP
FINYSIQKPCSPFDVDKPSSMQKQTQVKLRIQTDGDKYGGTSIQLQLKEKKKKGYCECCL
QKYEDLETHLLSEQHRNFAQSNQYQVVDDIVSKLVFDFVEYEKDTPKKKRIKYSVGSLSP
VSASVLKKTEQKEKVELQHISQKDCQEDDTTVKEQNFLYKETQETEKKLLFISEPIPHPS
NELRGLNEKMSNKCSMLSTAEDDIRQNFTQLPLHKNKQECILDISEHTLSENDLEELRVD
HYKCNIQASVHVSDFSTDNSGSQPKQKSDTVLFPAKDLKEKDLHSIFTHDSGLITINSSQ
EHLTVQAKAPFHTPPEEPNECDFKNMDSLPSGKIHRKVKIILGRNRKENLEPNAEFDKRT
EFITQEENRICSSPVQSLLDLFQTSEEKSEFLGFTSYTEKSGICNVLDIWEEENSDNLLT
AFFSSPSTSTFTGF
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Component 2 |
Name: | Cell division cycle 7-related protein kinase |
Synonyms: | CDC7 | CDC7-related kinase | CDC7L1 | CDC7_HUMAN | Cell division cycle 7-related protein kinase (CDC7) | HsCdc7 | huCdc7 |
Type: | Protein |
Mol. Mass.: | 63908.16 |
Organism: | Homo sapiens (Human) |
Description: | O00311 |
Residue: | 574 |
Sequence: | MEASLGIQMDEPMAFSPQRDRFQAEGSLKKNEQNFKLAGVKKDIEKLYEAVPQLSNVFKI
EDKIGEGTFSSVYLATAQLQVGPEEKIALKHLIPTSHPIRIAAELQCLTVAGGQDNVMGV
KYCFRKNDHVVIAMPYLEHESFLDILNSLSFQEVREYMLNLFKALKRIHQFGIVHRDVKP
SNFLYNRRLKKYALVDFGLAQGTHDTKIELLKFVQSEAQQERCSQNKSHIITGNKIPLSG
PVPKELDQQSTTKASVKRPYTNAQIQIKQGKDGKEGSVGLSVQRSVFGERNFNIHSSISH
ESPAVKLMKQSKTVDVLSRKLATKKKAISTKVMNSAVMRKTASSCPASLTCDCYATDKVC
SICLSRRQQVAPRAGTPGFRAPEVLTKCPNQTTAIDMWSAGVIFLSLLSGRYPFYKASDD
LTALAQIMTIRGSRETIQAAKTFGKSILCSKEVPAQDLRKLCERLRGMDSSTPKLTSDIQ
GHASHQPAISEKTDHKASCLVQTPPGQYSGNSFKKGDSNSCEHCFDEYNTNLEGWNEVPD
EAYDLLDKLLDLNPASRITAEEALLHPFFKDMSL
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BDBM158154 |
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n/a |
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Name | BDBM158154 |
Synonyms: | US10081622, Compound 11 | US10370379, Entrectinib | US11059827, Compound Entrectinib | US11267806, Compound T-12 | US9029356, 11 | US9255087, 11 | US9616059, 11 |
Type | Small organic molecule |
Emp. Form. | C31H34F2N6O2 |
Mol. Mass. | 560.6375 |
SMILES | CN1CCN(CC1)c1ccc(C(=O)Nc2n[nH]c3ccc(Cc4cc(F)cc(F)c4)cc23)c(NC2CCOCC2)c1 |
Structure |
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