Target
Tyrosine-protein kinase BTK
Ligand
BDBM377842
Substrate
n/a
Meas. Tech.
LanthaScreen Assay
IC50
7.80±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:
BDBM377842
Synonyms:
1-[(3S)-1-acryloyl piperidin-3-yl]-5-amino-3-[4-(2,4-difluorophenoxy)phenyl]-1H-pyrazole-4-carboxamide | US10266513, Example 136 | US10266513, Example 137 | US10815213, Example 137
Type:
Small organic molecule
Emp. Form.:
C24H23F2N5O3
Mol. Mass.:
467.4679
SMILES:
NC(=O)c1c(N)n(nc1-c1ccc(Oc2ccc(F)cc2F)cc1)C1CCCN(C1)C(=O)C=C
Structure:
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