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Target
Tyrosine-protein kinase BTK
Ligand
BDBM324336
Substrate
n/a
Meas. Tech.
In Vitro Kinase Assay
IC50
<1.000±n/a nM
Citation
Hopkins, BT; Ma, B; Prince, R; Marx, I; Lyssikatos, JP; Zheng, F; Peterson, M; Patience, DB Inhibiting agents for Bruton's tyrosine kinase US Patent US10961237 Publication Date 3/30/2021
More Info.:
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:
BDBM324336
Synonyms:
(R)-5-(tert-butyl)-N-(2- (cyclopropylmethyl)-8- (2-((1-methyl-1H- pyrazol-4- yl)amino)pyrimidin-4- yl)-2,3,4,5-tetrahydro- 1H-benzo[c]azepin-5- yl)-1,3,4-oxadiazole-2- carboxamide | US10189829, Compound 107 | US10227341, Compound 107 | US10961237, Compound 107 | US11858926, Compound 107
Type:
Small organic molecule
Emp. Form.:
C29H35N9O2
Mol. Mass.:
541.6473
SMILES:
Cn1cc(Nc2nccc(n2)-c2ccc3[C@@H](CCN(CC4CC4)Cc3c2)NC(=O)c2nnc(o2)C(C)(C)C)cn1 |r|