Reaction Details Report a problem with these data
Target
Tyrosine-protein kinase BTK
Ligand
BDBM610463
Substrate
n/a
Meas. Tech.
ChEMBL_2291580
IC50
>2000±n/a nM
Citation
Hartz, RA; Ahuja, VT; Sivaprakasam, P; Xiao, H; Krause, CM; Clarke, WJ; Kish, K; Lewis, H; Szapiel, N; Ravirala, R; Mutalik, S; Nakmode, D; Shah, D; Burton, CR; Macor, JE; Dubowchik, GM Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2- J Med Chem 66:4231-4252 (2023) [PubMed]
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:
BDBM610463
Synonyms:
BDBM610464 | BDBM610465 | N-(4-(2-Methylmorpholino)pyridin-3-yl)-2-phenylimidazo[1,2-b]pyridazine-8-carboxamide | US10774086, Example 14
Type:
Small organic molecule
Emp. Form.:
C23H22N6O2
Mol. Mass.:
414.4598
SMILES:
CC1CN(CCO1)c1ccncc1NC(=O)c1ccnn2cc(nc12)-c1ccccc1