Target
Tyrosine-protein kinase BTK
Ligand
BDBM324323
Substrate
n/a
Meas. Tech.
BTK-POLYGAT-LS ASSAY
IC50
<1.000±n/a nM
Citation
 Hopkins, BTMa, BPrince, RMarx, ILyssikatos, JPZheng, FPeterson, MPatience, DB Inhibiting agents for Bruton's tyrosine kinase US Patent  US10189829 Publication Date 1/29/2019 
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:
BDBM324323
Synonyms:
5-tert-butyl-1,3,4- oxadiazole-2-carboxylic acid {(R)-2-(2-hydroxy- 2-methyl-propyl)- 8-[2-(1- methyl-1H-pyrazol-4- ylamino)-pyrimidin-4- yl]-2,3,4,5-tetrahydro- 1H-2-benzazepin-5-yl}- amide | US10189829, Compound 89a | US10227341, Compound 89a | US10961237, Compound 89a | US11858926, Compound 89a
Type:
Small organic molecule
Emp. Form.:
C29H37N9O3
Mol. Mass.:
559.6626
SMILES:
Cn1cc(Nc2nccc(n2)-c2ccc3[C@@H](CCN(CC(C)(C)O)Cc3c2)NC(=O)c2nnc(o2)C(C)(C)C)cn1 |r|
Structure:
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