Target
Tyrosine-protein kinase BTK
Ligand
BDBM470491
Substrate
n/a
Meas. Tech.
LanthaScreen Assay
IC50
0.480±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:
BDBM470491
Synonyms:
1-[(3R)-1-acryloylpiperidin-3-yl]-5-amino-3-{4-[(5-chloro-3-fluoropyridin-2-yl)oxy]phenyl}-1H-pyrazole-4-carboxamide | US10815213, Example 153
Type:
Small organic molecule
Emp. Form.:
C23H22ClFN6O3
Mol. Mass.:
484.911
SMILES:
NC(=O)c1c(N)n(nc1-c1ccc(Oc2ncc(Cl)cc2F)cc1)[C@@H]1CCCN(C1)C(=O)C=C |r|
Structure:
Search PDB for entries with ligand similarity: