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Target
Cell division cycle 7-related protein kinase/Protein DBF4 homolog A
Ligand
BDBM158154
Substrate
n/a
Meas. Tech.
ChEMBL_1577171 (CHEMBL3807433)
IC50
>10000±n/a nM
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 Chem 59:3392-408 (2016) [PubMed]  Article 
Target
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:
MNSGAMRIHSKGHFQGGIQVKNEKNRPSLKSLKTDNRPEKSKCKPLWGKVFYLDLPSVTISEKLQKDIKDLGGRVEEFLSKDISYLISNKKEAKFAQTLGRISPVPSPESAYTAETTSPHPSHDGSSFKSPDTVCLSRGKLLVEKAIKDHDFIPSNSILSNALSWGVKILHIDDIRYYIEQKKKELYLLKKSSTSVRDGGKRVGSGAQKTRTGRLKKPFVKVEDMSQLYRPFYLQLTNMPFINYSIQKPCSPFDVDKPSSMQKQTQVKLRIQTDGDKYGGTSIQLQLKEKKKKGYCECCLQKYEDLETHLLSEQHRNFAQSNQYQVVDDIVSKLVFDFVEYEKDTPKKKRIKYSVGSLSPVSASVLKKTEQKEKVELQHISQKDCQEDDTTVKEQNFLYKETQETEKKLLFISEPIPHPSNELRGLNEKMSNKCSMLSTAEDDIRQNFTQLPLHKNKQECILDISEHTLSENDLEELRVDHYKCNIQASVHVSDFSTDNSGSQPKQKSDTVLFPAKDLKEKDLHSIFTHDSGLITINSSQEHLTVQAKAPFHTPPEEPNECDFKNMDSLPSGKIHRKVKIILGRNRKENLEPNAEFDKRTEFITQEENRICSSPVQSLLDLFQTSEEKSEFLGFTSYTEKSGICNVLDIWEEENSDNLLTAFFSSPSTSTFTGF
  
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:
MEASLGIQMDEPMAFSPQRDRFQAEGSLKKNEQNFKLAGVKKDIEKLYEAVPQLSNVFKIEDKIGEGTFSSVYLATAQLQVGPEEKIALKHLIPTSHPIRIAAELQCLTVAGGQDNVMGVKYCFRKNDHVVIAMPYLEHESFLDILNSLSFQEVREYMLNLFKALKRIHQFGIVHRDVKPSNFLYNRRLKKYALVDFGLAQGTHDTKIELLKFVQSEAQQERCSQNKSHIITGNKIPLSGPVPKELDQQSTTKASVKRPYTNAQIQIKQGKDGKEGSVGLSVQRSVFGERNFNIHSSISHESPAVKLMKQSKTVDVLSRKLATKKKAISTKVMNSAVMRKTASSCPASLTCDCYATDKVCSICLSRRQQVAPRAGTPGFRAPEVLTKCPNQTTAIDMWSAGVIFLSLLSGRYPFYKASDDLTALAQIMTIRGSRETIQAAKTFGKSILCSKEVPAQDLRKLCERLRGMDSSTPKLTSDIQGHASHQPAISEKTDHKASCLVQTPPGQYSGNSFKKGDSNSCEHCFDEYNTNLEGWNEVPDEAYDLLDKLLDLNPASRITAEEALLHPFFKDMSL
  
Inhibitor
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:
Search PDB for entries with ligand similarity: