Target
Tyrosine-protein kinase BTK
Ligand
BDBM377734
Substrate
n/a
Meas. Tech.
LanthaScreen Assay
IC50
0.430±n/a nM
Citation
 Springer, JRDevadas, BGarland, DJGrapperhaus, MLHan, SHockerman, SLHughes, ROSaiah, ESchnute, MESelness, SRWalker, DPWan, ZXing, LZapf, CWSchmidt, MA Bruton's tyrosine kinase inhibitors US Patent  US10815213 Publication Date 10/27/2020 
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:
BDBM377734
Synonyms:
5-amino-1-(1-cyanopiperidin-3-yl)-3-[4-(3-fluoro-4-methylphenoxy)phenyl]-1H-pyrazole-4-carboxamide | US10266513, Example 28 | US10266513, Example 29 | US10266513, Example 30 | US10815213, Example 30
Type:
Small organic molecule
Emp. Form.:
C23H23FN6O2
Mol. Mass.:
434.4661
SMILES:
Cc1ccc(Oc2ccc(cc2)-c2nn(C3CCCN(C3)C#N)c(N)c2C(N)=O)cc1F
Structure:
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