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Target
Serine/threonine-protein kinase Nek8
Ligand
BDBM2579
Substrate
n/a
Meas. Tech.
ChEMBL_1828656 (CHEMBL4328530)
IC50
17.5±n/a nM
Citation
 Narayan, S; Ramisetti, S; Jaiswal, AS; Law, BK; Singh-Pillay, A; Singh, P; Amin, S; Sharma, AK ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells. Eur J Med Chem 161:456-467 (2019) [PubMed]  Article 
Target
Name:
Serine/threonine-protein kinase Nek8
Synonyms:
2.7.11.1 | Never in mitosis A-related kinase 8 | NimA-related protein kinase 8 | Nima-related protein kinase 12a | Serine/threonine-protein kinase Nek8 | NEK8_HUMAN | NEK8 | JCK | NEK12A
Type:
PROTEIN
Mol. Mass.:
74819.06
Organism:
Human
Description:
ChEMBL_119768
Residue:
692
Sequence:
MEKYERIRVVGRGAFGIVHLCLRKADQKLVIIKQIPVEQMTKEERQAAQNECQVLKLLNHPNVIEYYENFLEDKALMIAMEYAPGGTLAEFIQKRCNSLLEEETILHFFVQILLALHHVHTHLILHRDLKTQNILLDKHRMVVKIGDFGISKILSSKSKAYTVVGTPCYISPELCEGKPYNQKSDIWALGCVLYELASLKRAFEAANLPALVLKIMSGTFAPISDRYSPELRQLVLSLLSLEPAQRPPLSHIMAQPLCIRALLNLHTDVGSVRMRRAEKSVAPSNTGSRTTSVRCRGIPRGPVRPAIPPPLSSVYAWGGGLGTPLRLPMLNTEVVQVAAGRTQKAGVTRSGRLILWEAPPLGAGGGSLLPGAVEQPQPQFISRFLEGQSGVTIKHVACGDFFTACLTDRGIIMTFGSGSNGCLGHGSLTDISQPTIVEALLGYEMVQVACGASHVLALSTERELFAWGRGDSGRLGLGTRESHSCPQQVPMPPGQEAQRVVCGIDSSMILTVPGQALACGSNRFNKLGLDHLSLGEEPVPHQQVEEALSFTLLGSAPLDQEPLLSIDLGTAHSAAVTASGDCYTFGSNQHGQLGTNTRRGSRAPCKVQGLEGIKMAMVACGDAFTVAIGAESEVYSWGKGARGRLGRRDEDAGLPRPVQLDETHPYTVTSVSCCHGNTLLAVRSVTDEPVPP
  
Inhibitor
Name:
BDBM2579
Synonyms:
CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 | (2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one | Staurosporine | US9206188, Staurosporine | US9226923, Staurosporine | US20240002365, Compound staurosporine | US11958831, Example Staurosporine | US20240254124, Compound Staurosporine | US20240309004, Compound STAUROSPORINE | US12350272, Compound Staurosporine | US12398142, Compound Staurosporine | US12410173, Compound Staurosporine
Type:
Small organic molecule
Emp. Form.:
C28H26N4O3
Mol. Mass.:
466.20
SMILES:
C[C@@]12[C@@H]([C@@H](C[C@@H](O1)n3c4ccccc4c5c3c6n2c7ccccc7c6c8c5C(=O)NC8)NC)OC
Structure:
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