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Target
Tyrosine-protein kinase BTK
Ligand
BDBM441027
Substrate
n/a
Meas. Tech.
Inhibition TR-FRET (Time Resolved FRET) Assay
IC50
41.0±n/a nM
Citation
 Frattini, S; Bakker, R; Giovannini, R; Fossati, G; Hamprecht, D; Lingard, I; Pautsch, A; Wellenzohn, B Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors US Patent  US10640486 Publication Date 5/5/2020 
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:
BDBM441027
Synonyms:
1-{1-[6-(3-Aza-bicyclo[3.1.0]hex-3-yl)-pyridin-3-yl]-cyclopropyl}-1H-pyrazole-4-carboxylic acid ((R)-1-amino-6,7-dihydro-5H-[2]pyrindin-5-yl)amide | US10640486, Example 74
Type:
Small organic molecule
Emp. Form.:
C25H27N7O
Mol. Mass.:
441.5282
SMILES:
Nc1nccc2[C@@H](CCc12)NC(=O)c1cnn(c1)C1(CC1)c1ccc(nc1)N1CC2CC2C1 |r|
Structure:
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