Reaction Details |
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Target | Cyclin-dependent kinase 5 activator 1 |
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Ligand | BDBM50307987 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_608387 (CHEMBL1074421) |
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IC50 | 140±n/a nM |
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Citation | Brasca, MG; Albanese, C; Alzani, R; Amici, R; Avanzi, N; Ballinari, D; Bischoff, J; Borghi, D; Casale, E; Croci, V; Fiorentini, F; Isacchi, A; Mercurio, C; Nesi, M; Orsini, P; Pastori, W; Pesenti, E; Pevarello, P; Roussel, P; Varasi, M; Volpi, D; Vulpetti, A; Ciomei, M Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing. Bioorg Med Chem18:1844-53 (2010) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Cyclin-dependent kinase 5 activator 1 |
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Name: | Cyclin-dependent kinase 5 activator 1 |
Synonyms: | CDK5/p35 | Cyclin-Dependent Kinase 5 (CDK5) | Cyclin-dependent kinase 5 regulatory subunit 1 | Cyclin-dependent kinase 5/CDK5 activator 1 |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
Name: | Cyclin-dependent kinase 5 |
Synonyms: | CDK5 | CDK5_HUMAN | CDKN5 | Cell division protein kinase 5 | Cyclin-dependent kinase 5 (CDK5/ p25) | Cyclin-dependent kinase 5 (CDK5/p35) | Cyclin-dependent-like kinase 5 | Cyclin-dependent-like kinase 5 (CDK5) | PSSALRE | Serine/threonine-protein kinase PSSALRE | Tau protein kinase II catalytic subunit |
Type: | Enzyme Subunit |
Mol. Mass.: | 33308.61 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 292 |
Sequence: | MQKYEKLEKIGEGTYGTVFKAKNRETHEIVALKRVRLDDDDEGVPSSALREICLLKELKH
KNIVRLHDVLHSDKKLTLVFEFCDQDLKKYFDSCNGDLDPEIVKSFLFQLLKGLGFCHSR
NVLHRDLKPQNLLINRNGELKLADFGLARAFGIPVRCYSAEVVTLWYRPPDVLFGAKLYS
TSIDMWSAGCIFAELANAGRPLFPGNDVDDQLKRIFRLLGTPTEEQWPSMTKLPDYKPYP
MYPATTSLVNVVPKLNATGRDLLQNLLKCNPVQRISAEEALQHPYFSDFCPP
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Component 2 |
Name: | Cyclin-dependent kinase 5 activator 1 |
Synonyms: | CD5R1_HUMAN | CDK5R | CDK5R1 | Cyclin-Dependent Kinase 5 Activator 1, p35 | Cyclin-dependent kinase 5 (CDK5/p25) | Cyclin-dependent kinase 5 regulatory subunit 1 | NCK5A | TPKII regulatory subunit | p35 |
Type: | Enzyme Subunit |
Mol. Mass.: | 34077.43 |
Organism: | Homo sapiens (Human) |
Description: | Q15078 |
Residue: | 307 |
Sequence: | MGTVLSLSPSYRKATLFEDGAATVGHYTAVQNSKNAKDKNLKRHSIISVLPWKRIVAVSA
KKKNSKKVQPNSSYQNNITHLNNENLKKSLSCANLSTFAQPPPAQPPAPPASQLSGSQTG
GSSSVKKAPHPAVTSAGTPKRVIVQASTSELLRCLGEFLCRRCYRLKHLSPTDPVLWLRS
VDRSLLLQGWQDQGFITPANVVFLYMLCRDVISSEVGSDHELQAVLLTCLYLSYSYMGNE
ISYPLKPFLVESCKEAFWDRCLSVINLMSSKMLQINADPHYFTQVFSDLKNESGQEDKKR
LLLGLDR
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BDBM50307987 |
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n/a |
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Name | BDBM50307987 |
Synonyms: | CHEMBL604712 | N-[5-(2,2-Dimethylpropanoyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl]-3,5-difluorobenzamide |
Type | Small organic molecule |
Emp. Form. | C19H22F2N4O2 |
Mol. Mass. | 376.4004 |
SMILES | CC(C)(C)C(=O)N1Cc2c(NC(=O)c3cc(F)cc(F)c3)[nH]nc2C1(C)C |
Structure |
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