Reaction Details |
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Target | Cyclin-dependent kinase 5 activator 1 |
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Ligand | BDBM50343559 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_747264 (CHEMBL1776523) |
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IC50 | >10000±n/a nM |
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Citation | Beria, I; Bossi, RT; Brasca, MG; Caruso, M; Ceccarelli, W; Fachin, G; Fasolini, M; Forte, B; Fiorentini, F; Pesenti, E; Pezzetta, D; Posteri, H; Scolaro, A; Re Depaolini, S; Valsasina, B NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg Med Chem Lett21:2969-74 (2011) [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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BDBM50343559 |
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n/a |
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Name | BDBM50343559 |
Synonyms: | 1-(2-HYDROXYETHYL)-8-[[5-(4-METHYLPIPERAZIN-1-YL)-2-(TRIFLUOROMETHOXY)PHENYL]AMINO]-4,5-DIHYDROPYRIMIDO[5,4-G]INDAZOLE-3-CARBOXAMIDE | 1-(2-hydroxyethyl)-8-(5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1738758 |
Type | Small organic molecule |
Emp. Form. | C24H27F3N8O3 |
Mol. Mass. | 532.5182 |
SMILES | CN1CCN(CC1)c1ccc(OC(F)(F)F)c(Nc2ncc3CCc4c(nn(CCO)c4-c3n2)C(N)=O)c1 |
Structure |
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