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Target
Tyrosine-protein kinase BTK
Ligand
BDBM662960
Substrate
n/a
Meas. Tech.
Electrophoretic Mobility Shift Assay (MSA)
IC50
0.053±n/a nM
Citation
 Bian, Z; Burke, JP; Jia, ZJ; Jiang, X; Katcher, MH; Mali, VR; Marin, VL; Noey, EL; Okano, A; Rivkin, AA; Scholz, SO; Woller, KR; Zhao, X; Adams, AM; Biannic, B; Mortezaei, S; Payette, JN; Zablocki, JA PYRIMIDINES FOR DEGRADING BRUTON'S TYROSINE KINASE US Patent  US20240109877 Publication Date 4/4/2024
Target
Name:
Tyrosine-protein kinase BTK
Synonyms:
AGMX1 | ATK | Agammaglobulinaemia tyrosine kinase | Agammaglobulinemia tyrosine kinase | B cell progenitor kinase | B-cell progenitor kinase | BPK | BTK | BTK_HUMAN | Bruton tyrosine kinase | Tyrosine Kinase BTK | Tyrosine-protein kinase (BTK) | Tyrosine-protein kinase BTK (BTK)
Type:
Enzyme
Mol. Mass.:
76289.95
Organism:
Homo sapiens (Human)
Description:
Q06187
Residue:
659
Sequence:
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVFAKSTGDPQGVIRHYVVCSTPQSQYYLAEKHLFSTIPELINYHQHNSAGLISRLKYPVSQQNKNAPSTAGLGYGSWEIDPKDLTFLKELGTGQFGVVKYGKWRGQYDVAIKMIKEGSMSEDEFIEEAKVMMNLSHEKLVQLYGVCTKQRPIFIITEYMANGCLLNYLREMRHRFQTQQLLEMCKDVCEAMEYLESKQFLHRDLAARNCLVNDQGVVKVSDFGLSRYVLDDEYTSSVGSKFPVRWSPPEVLMYSKFSSKSDIWAFGVLMWEIYSLGKMPYERFTNSETAEHIAQGLRLYRPHLASEKVYTIMYSCWHEKADERPTFKILLSNILDVMDEES
  
Inhibitor
Name:
BDBM662960
Synonyms:
US20240109877, Example 14
Type:
Small organic molecule
Emp. Form.:
C41H46ClN11O4
Mol. Mass.:
792.328
SMILES:
C[C@@H](NC(=O)c1nc(no1)C(C)(C)C)c1ccc(cc1Cl)-c1cc(Nc2ccc(cn2)N2CCN(CCc3ccc(cc3)N3CCC(=O)NC3=O)C[C@@H]2C)ncn1 |r|
Structure:
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