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Target
Tyrosine-protein kinase BTK
Ligand
BDBM377762
Substrate
n/a
Meas. Tech.
LanthaScreen Assay
IC50
1.30±n/a nM
Citation
Springer, JR; Devadas, B; Garland, DJ; Grapperhaus, ML; Han, S; Hockerman, SL; Hughes, RO; Saiah, E; Schnute, ME; Selness, SR; Walker, DP; Wan, Z; Xing, L; Zapf, CW; Schmidt, MA Bruton's tyrosine kinase inhibitors US Patent US10815213 Publication Date 10/27/2020
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:
BDBM377762
Synonyms:
5-amino-3-[4-(2-chlorophenoxy)- phenyl]-1-(1-cyanopiperidin-3-yl)- 1H-pyrazole-4-carboxamide | US10266513, Example 56 | US10815213, Example 56
Type:
Small organic molecule
Emp. Form.:
C22H21ClN6O2
Mol. Mass.:
436.894
SMILES:
NC(=O)c1c(N)n(nc1-c1ccc(Oc2ccccc2Cl)cc1)C1CCCN(C1)C#N