Target
Tyrosine-protein kinase BTK
Ligand
BDBM377809
Substrate
n/a
Meas. Tech.
Human BTK LanthaScreen Assay
IC50
13.4±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  US10266513 Publication Date 4/23/2019 
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:
BDBM377809
Synonyms:
5-amino-3-[3-(3-chloro-4- methylphenoxy)-phenyl]-1-(1- cyanopiperidin-3-yl)-1H-pyrazole- 4-carboxamide | US10266513, Example 103 | US10815213, Example 103
Type:
Small organic molecule
Emp. Form.:
C23H23ClN6O2
Mol. Mass.:
450.921
SMILES:
Cc1cccc(Oc2cccc(c2)-c2nn(C3CCCN(C3)C#N)c(N)c2C(N)=O)c1Cl
Structure:
Search PDB for entries with ligand similarity: