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Target
Serine/threonine-protein kinase tousled-like 1
Ligand
BDBM8226
Substrate
n/a
Meas. Tech.
ChEMBL_2130021 (CHEMBL4839450)
IC50
13000±n/a nM
Citation
 Serafim, RAM; Sorrell, FJ; Berger, BT; Collins, RJ; Vasconcelos, SNS; Massirer, KB; Knapp, S; Bennett, J; Fedorov, O; Patel, H; Zuercher, WJ; Elkins, JM Discovery of a Potent Dual SLK/STK10 Inhibitor Based on a Maleimide Scaffold. J Med Chem 64:13259-13278 (2021) [PubMed]  Article 
Target
Name:
Serine/threonine-protein kinase tousled-like 1
Synonyms:
KIAA0137 | Serine/threonine-protein kinase tousled-like 1 | TLK1 | TLK1_HUMAN
Type:
Enzyme Catalytic Domain
Mol. Mass.:
86722.30
Organism:
Homo sapiens (Human)
Description:
gi_33636698
Residue:
766
Sequence:
MSVQSSSGSLEGPPSWSQLSTSPTPGSAAAARSLLNHTPPSGRPREGAMDELHSLDPRRQELLEARFTGVASGSTGSTGSCSVGAKASTNNESSNHSFGSLGSLSDKESETPEKKQSESSRGRKRKAENQNESSQGKSIGGRGHKISDYFEYQGGNGSSPVRGIPPAIRSPQNSHSHSTPSSSVRPNSPSPTALAFGDHPIVQPKQLSFKIIQTDLTMLKLAALESNKIQDLEKKEGRIDDLLRANCDLRRQIDEQQKLLEKYKERLNKCISMSKKLLIEKSTQEKLSSREKSMQDRLRLGHFTTVRHGASFTEQWTDGFAFQNLVKQQEWVNQQREDIERQRKLLAKRKPPTANNSQAPSTNSEPKQRKNKAVNGAENDPFVRPNLPQLLTLAEYHEQEEIFKLRLGHLKKEEAEIQAELERLERVRNLHIRELKRINNEDNSQFKDHPTLNERYLLLHLLGRGGFSEVYKAFDLYEQRYAAVKIHQLNKSWRDEKKENYHKHACREYRIHKELDHPRIVKLYDYFSLDTDTFCTVLEYCEGNDLDFYLKQHKLMSEKEARSIVMQIVNALRYLNEIKPPIIHYDLKPGNILLVDGTACGEIKITDFGLSKIMDDDSYGVDGMDLTSQGAGTYWYLPPECFVVGKEPPKISNKVDVWSVGVIFFQCLYGRKPFGHNQSQQDILQENTILKATEVQFPVKPVVSSEAKAFIRRCLAYRKEDRFDVHQLANDPYLLPHMRRSNSSGNLHMAGLTASPTPPSSSIITY
  
Inhibitor
Name:
BDBM8226
Synonyms:
3-[(3-chlorophenyl)amino]-4-(2-methoxyphenyl)-2,5-dihydro-1H-pyrrole-2,5-dione | 4-arylmaleimide deriv. 6i
Type:
Small organic molecule
Emp. Form.:
C17H13ClN2O3
Mol. Mass.:
328.75
SMILES:
COc1ccccc1C1=C(Nc2cccc(Cl)c2)C(=O)NC1=O |c:9|
Structure:
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