Protein Information

General Information of the Protein

Protein ID	PT01308
Protein Name	Tyrosine-protein kinase BTK
Secondarily Protein Name	Agammaglobulinemia tyrosine kinase B-cell progenitor kinase Bruton tyrosine kinase
Gene Name	BTK
Secondarily Gene Name	AGMX1 ATK BPK
Sequence	MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVFAKSTGDPQGVIRHYVVCSTPQSQYYLAEKHLFSTIPELINYHQHNSAGLISRLKYPVSQQNKNAPSTAGLGYGSWEIDPKDLTFLKELGTGQFGVVKYGKWRGQYDVAIKMIKEGSMSEDEFIEEAKVMMNLSHEKLVQLYGVCTKQRPIFIITEYMANGCLLNYLREMRHRFQTQQLLEMCKDVCEAMEYLESKQFLHRDLAARNCLVNDQGVVKVSDFGLSRYVLDDEYTSSVGSKFPVRWSPPEVLMYSKFSSKSDIWAFGVLMWEIYSLGKMPYERFTNSETAEHIAQGLRLYRPHLASEKVYTIMYSCWHEKADERPTFKILLSNILDVMDEES Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme > Kinase > Protein Kinase > TK protein kinase group > Tyrosine protein kinase Tec family
Function	Non-receptor tyrosine kinase indispensable for B lymphocyte development, differentiation and signaling (PubMed:19290921). Binding of antigen to the B-cell antigen receptor (BCR) triggers signaling that ultimately leads to B-cell activation (PubMed:19290921). After BCR engagement and activation at the plasma membrane, phosphorylates PLCG2 at several sites, igniting the downstream signaling pathway through calcium mobilization, followed by activation of the protein kinase C (PKC) family members (PubMed:11606584). PLCG2 phosphorylation is performed in close cooperation with the adapter protein B-cell linker protein BLNK (PubMed:11606584). BTK acts as a platform to bring together a diverse array of signaling proteins and is implicated in cytokine receptor signaling pathways (PubMed:16517732, PubMed:17932028). Plays an important role in the function of immune cells of innate as well as adaptive immunity, as a component of the Toll-like receptors (TLR) pathway (PubMed:16517732). The TLR pathway acts as a primary surveillance system for the detection of pathogens and are crucial to the activation of host defense (PubMed:16517732). Especially, is a critical molecule in regulating TLR9 activation in splenic B-cells (PubMed:16517732, PubMed:17932028). Within the TLR pathway, induces tyrosine phosphorylation of TIRAP which leads to TIRAP degradation (PubMed:16415872). BTK also plays a critical role in transcription regulation (PubMed:19290921). Induces the activity of NF-kappa-B, which is involved in regulating the expression of hundreds of genes (PubMed:19290921). BTK is involved on the signaling pathway linking TLR8 and TLR9 to NF-kappa-B (PubMed:19290921). Acts as an activator of NLRP3 inflammasome assembly by mediating phosphorylation of NLRP3 (PubMed:34554188). Transiently phosphorylates transcription factor GTF2I on tyrosine residues in response to BCR (PubMed:9012831). GTF2I then translocates to the nucleus to bind regulatory enhancer elements to modulate gene expression (PubMed:9012831). ARID3A and NFAT are other transcriptional target of BTK (PubMed:16738337). BTK is required for the formation of functional ARID3A DNA-binding complexes (PubMed:16738337). There is however no evidence that BTK itself binds directly to DNA (PubMed:16738337). BTK has a dual role in the regulation of apoptosis (PubMed:9751072). Show/Hide
Uniprot ID	Primary ID: Q06187 Secondarily ID: B2RAW1 Q32ML5 Show/Hide
Ensembl ID	ENSG00000010671
HGNC ID	HGNC:1133
Subcellular Location	Cytoplasm Cell membrane Nucleus Membrane raft

Map of Molecular Bioactivity Related to the Protein

Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity

Table of Molecular Bioactivities Related to the Protein

Cell Line ID: CL000025 , HEK-293T

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0414116 Compound Info	4-tert-butyl-N-[2-methyl-3-[1-methyl-5-[4-(morpholine-4-carbonyl)-3-(prop-2-enoylamino)anilino]-6-oxopyridin-3-yl]phenyl]benzamide Show/Hide	C38H41N5O5	2
1	EC50 = 4.7 nM Bioactivity Info	TI LI LO TS
2	EC50 > 100 nM Bioactivity Info	TI LI LO TS
CP0447342 Compound Info	4-tert-butyl-N-[2-methyl-3-[1-methyl-5-[4-(morpholine-4-carbonyl)-3-(propanoylamino)anilino]-6-oxopyridin-3-yl]phenyl]benzamide Show/Hide	C38H43N5O5	1
1	EC50 > 100 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000549 , Namalwa

Cell Line Info

Cell Line ID: CL000752 , PBMC iPSC #1

Cell Line Info

Cell Line ID: CL000176 , Pfeiffer

Cell Line Info

Cell Line ID: CL000174 , Raji

Cell Line Info

Cell Line ID: CL000003 , Ramos

Cell Line Info

Cell Line ID: CL000012 , Sf21

Cell Line Info

Cell Line ID: CL000013 , Sf9

Cell Line Info

Cell Line ID: CL000040 , THP-1

Cell Line Info

Cell Line ID: CL000222 , TMD8

Cell Line Info

Cell Line ID: CL000177 , U-2932

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0812674 Compound Info	(S)-5-Fluoro-2,3-dimethyl-4-(3-propiolamidopiperidin-1-yl)-1H-indole-7-carboxamide Show/Hide	C19H21FN4O2	1
1	IC50 = 0.07 nM
CP0007430 Compound Info	IBRUTINIB Show/Hide	C25H24N6O2	32
1	IC50 = 0.08 nM
2	IC50 = 0.11 nM
3	IC50 = 0.2 nM
4	IC50 = 0.21 nM
5	IC50 = 0.33 nM
6	IC50 = 0.4 nM
7	IC50 = 0.42 nM
8	IC50 = 0.46 nM
9	IC50 <= 0.5 nM
10	IC50 = 0.5 nM
11	IC50 < 0.5 nM
12	IC50 = 0.54 nM
13	IC50 = 0.6 nM
14	IC50 = 0.64 nM
15	IC50 = 0.7 nM
16	IC50 = 0.72 nM
17	IC50 = 0.8 nM
18	IC50 = 0.89 nM
19	IC50 = 1 nM
20	IC50 = 1.2 nM
21	IC50 = 1.5 nM
22	IC50 = 2.2 nM
23	IC50 = 2.3 nM
24	IC50 = 4 nM
25	IC50 = 5 nM
26	IC50 = 12.9 nM
27	IC50 = 14 nM
28	IC50 = 810 nM
29	IC50 = 1002 nM
30	Kd = 0.64 nM
31	Kd = 1.9 nM
32	Ki = 425 nM
CP0694113 Compound Info	BRANEBRUTINIB Show/Hide	C20H23FN4O2	3
1	IC50 = 0.1 nM
2	Kd = 0.56 nM
3	Ki = 116 nM
CP0070022 Compound Info	US10005782, Compound 136 Show/Hide	C26H25N5O3	1
1	IC50 = 0.13 nM
CP0361457 Compound Info	US10005782, Compound 52 Show/Hide	C24H21N5O3	1
1	IC50 = 0.14 nM
CP0878825 Compound Info	(S)-2,3-Dimethyl-4-(3-propiolamidopiperidin-1-yl)-1H-indole-7-carboxamide Show/Hide	C19H22N4O2	1
1	IC50 = 0.14 nM
CP0163693 Compound Info	US10005782, Compound 123 Show/Hide	C25H23N5O3	1
1	IC50 = 0.15 nM
CP0525585 Compound Info	US10138229, Example 54 Show/Hide	C24H25N5O3	1
1	IC50 = 0.17 nM
CP0063954 Compound Info	US10005782, Compound 63 Show/Hide	C24H21N5O3	1
1	IC50 = 0.18 nM
CP0350897 Compound Info	US10005782, Compound 54 Show/Hide	C27H28N6O3	1
1	IC50 = 0.19 nM
CP0490875 Compound Info	US9481682, 105 Show/Hide	C34H29F3N8O3	1
1	IC50 = 0.2 nM
CP0559443 Compound Info	US9481682, 85 Show/Hide	C34H30F3N9O4	1
1	IC50 = 0.2 nM
CP0569074 Compound Info	N-[2-[4-amino-6-[3-methyl-4-[[4-(2-methylpropyl)-2-oxopiperazin-1-yl]methyl]phenyl]pyrimidin-5-yl]oxyethyl]-N-methylprop-2-enamide Show/Hide	C26H36N6O3	2
1	IC50 = 0.22 nM
2	Kd = 0.91 nM
CP0117831 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]isoquinolin-1-one Show/Hide	C35H35FN6O3	7
1	IC50 = 0.3 nM
2	IC50 = 0.9 nM
3	IC50 = 2.25 nM
4	IC50 = 4 nM
5	IC50 = 7 nM
6	IC50 = 13 nM
7	IC50 = 13.2 nM
CP0260259 Compound Info	(E)-2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-(4-methylpiperazin-1-yl)pent-2-enenitrile Show/Hide	C34H38FN9O2	1
1	IC50 = 0.3 nM
CP0060760 Compound Info	US9447106, 27b (peak 2) Show/Hide	C27H29N5O3	7
1	IC50 = 0.3 nM
2	IC50 = 0.5 nM
3	IC50 = 0.92 nM
4	IC50 = 1.8 nM
5	IC50 = 2 nM
6	IC50 = 3.5 nM
7	Kd = 4.6 nM
CP0234526 Compound Info	US10005782, Compound 67 Show/Hide	C25H19N5O3	1
1	IC50 = 0.32 nM
CP0168515 Compound Info	US9447106, 27a (peak 1) Show/Hide	C27H29N5O3	1
1	IC50 = 0.33 nM
CP0440278 Compound Info	US10005782, Compound 121 Show/Hide	C25H23N5O3	1
1	IC50 = 0.36 nM
CP0387125 Compound Info	2-[3-[4-amino-6-[(1-methylpyrazol-4-yl)amino]-1,3,5-triazin-2-yl]-2-(hydroxymethyl)phenyl]-6-cyclopropyl-8-fluoroisoquinolin-1-one Show/Hide	C26H23FN8O2	3
1	IC50 = 0.39 nM
2	IC50 < 1 nM
3	IC50 = 4.2 nM
CP0110810 Compound Info	N-[(7S)-4-amino-6-methylidene-5-(4-phenoxyphenyl)-7,8-dihydropyrimido[5,4-b]pyrrolizin-7-yl]prop-2-enamide Show/Hide	C25H21N5O2	1
1	IC50 = 0.4 nM
CP0088490 Compound Info	US10894048, Ref. Ex Comp. 1 Show/Hide	C25H24N6O2	3
1	IC50 = 0.5 nM
2	IC50 = 1.4 nM
3	IC50 = 19 nM
CP0329552 Compound Info	5-amino-1-[(3R)-1-cyanopiperidin-3-yl]-3-[4-(2,4-difluorophenoxy)phenyl]pyrazole-4-carboxamide Show/Hide	C22H20F2N6O2	1
1	IC50 = 0.5 nM
CP0353769 Compound Info	(R)-1-(tert-butyl)-N-(8-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-2-(oxetan-3-yl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-5-yl)-1H-1,2,3-triazole-4-carboxamide Show/Hide	C28H34N10O2	1
1	IC50 < 0.5 nM
CP0688211 Compound Info	(S)-4-(3-(But-2-ynamido)piperidin-1-yl)-2,3-dimethyl-1H-indole-7-carboxamide Show/Hide	C20H24N4O2	1
1	IC50 = 0.52 nM
CP0699071 Compound Info	(S)-2,3-Dimethyl-4-(3-(vinylsulfonamido)piperidin-1-yl)-1H-indole-7-carboxamide Show/Hide	C18H24N4O3S	1
1	IC50 = 0.6 nM
CP0230300 Compound Info	5-amino-3-[4-(4-chlorophenoxy)phenyl]-1-[(3R)-1-cyanopiperidin-3-yl]pyrazole-4-carboxamide Show/Hide	C22H21ClN6O2	1
1	IC50 = 0.64 nM
CP0290996 Compound Info	7-(1,2-dihydroxyethyl)-4-[3-(6-fluoro-4-oxoquinazolin-3-yl)-2-methylphenyl]-9H-carbazole-1-carboxamide Show/Hide	C30H23FN4O4	1
1	IC50 = 0.7 nM
CP0689377 Compound Info	SPEBRUTINIB Show/Hide	C22H22FN5O3	3
1	IC50 = 0.7 nM
2	IC50 = 1 nM
3	IC50 = 4.61 nM
CP0178973 Compound Info	2-(4-phenoxyphenoxy)-6-[(1S,4S)-5-prop-2-enoyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]pyridine-3-carboxamide Show/Hide	C26H24N4O4	2
1	IC50 = 0.7 nM
2	IC50 = 82 nM
CP0562578 Compound Info	N-[[2-fluoro-4-[5-(1-prop-2-enoyl-3,6-dihydro-2H-pyridin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]methyl]benzamide Show/Hide	C28H24FN5O2	1
1	IC50 = 0.7 nM
CP0118878 Compound Info	US10005782, Compound 6b Show/Hide	C28H25N5O3	1
1	IC50 = 0.71 nM
CP0168514 Compound Info	US10005782, Compound 134b Show/Hide	C22H20ClN5O2	1
1	IC50 = 0.78 nM
CP0115507 Compound Info	US10604504, Example 114 Show/Hide	C19H22N4O2	1
1	IC50 = 0.85 nM
CP0260655 Compound Info	2-(3-{2-amino-6-[1-(oxetan-3-yl)-1,2,3,6-tetrahydropyridin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}-2-(hydroxymethyl)phenyl)-6-cyclopropyl-8-fluoroisoquinolin-1(2H)-one Show/Hide	C33H31FN6O3	4
1	IC50 = 0.85 nM
2	IC50 = 0.99 nM
3	IC50 = 3.72 nM
4	IC50 = 5.88 nM
CP0332245 Compound Info	4-[4-[[5-fluoro-4-[3-(prop-2-enoylamino)anilino]pyrimidin-2-yl]amino]phenoxy]-N-methylpyridine-2-carboxamide Show/Hide	C26H22FN7O3	1
1	IC50 < 1 nM
CP0070026 Compound Info	US10005782, Compound 27b Show/Hide	C27H29N5O3	1
1	IC50 = 1 nM
CP0053964 Compound Info	(7S)-3-fluoro-4-[3-(8-fluoro-1-methyl-2,4-dioxoquinazolin-3-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-6,7,8,9-tetrahydro-5H-carbazole-1-carboxamide Show/Hide	C32H30F2N4O4	1
1	IC50 = 1 nM
CP0537171 Compound Info	N-[[2-methyl-4-[2-[(1-methylpyrazol-4-yl)amino]pyrimidin-4-yl]phenyl]methyl]-3-propan-2-yloxyazetidine-1-carboxamide Show/Hide	C23H29N7O2	1
1	IC50 = 1 nM
CP0959369 Compound Info	(R)-2,3-Dimethyl-4-(3-(vinylsulfonamido)piperidin-1-yl)-1H-indole-7-carboxamide Show/Hide	C18H24N4O3S	1
1	IC50 = 1.2 nM
CP0005166 Compound Info	BMS-354825 Show/Hide	C22H26ClN7O2S	4
1	IC50 = 1.3 nM
2	IC50 = 3 nM
3	IC50 = 5 nM
4	Kd = 1.4 nM
CP0412987 Compound Info	US10005782, Compound 18 Show/Hide	C27H29N5O3	1
1	IC50 = 1.3 nM
CP0079085 Compound Info	2-[4-[(2S,6R)-2,6-dimethylmorpholin-4-yl]anilino]-6-[(3S)-3-(prop-2-enoylamino)pyrrolidin-1-yl]pyridine-3-carboxamide Show/Hide	C25H32N6O3	2
1	IC50 = 1.3 nM
2	IC50 = 52 nM
CP0842279 Compound Info	(RS)-2,3-Dimethyl-4-(3-(vinylsulfonamido)piperidin-1-yl)-1H-indole-7-carboxamide Show/Hide	C18H24N4O3S	1
1	IC50 = 1.4 nM
CP0959604 Compound Info	(R)-2,3-Dimethyl-4-(3-propiolamidopiperidin-1-yl)-1H-indole-7-carboxamide Show/Hide	C19H22N4O2	1
1	IC50 = 1.4 nM
CP0255832 Compound Info	US9481682, 121 Show/Hide	C30H28F3N7O3	1
1	IC50 = 1.4 nM
CP0163694 Compound Info	US10005782, Compound 164 Show/Hide	C23H23N5O2	1
1	IC50 = 1.6 nM
CP0168513 Compound Info	US10005782, Compound 20b Show/Hide	C26H27N5O3	1
1	IC50 = 1.6 nM
CP0713342 Compound Info	(S)-4-((1-Acryloylpyrrolidin-3-yl)amino)-2,3-dimethyl-1H-indole-7-carboxamide Show/Hide	C18H22N4O2	1
1	IC50 = 1.6 nM
CP0097627 Compound Info	(E)-2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4,4-dimethylpent-2-enenitrile Show/Hide	C30H30FN7O2	2
1	IC50 = 1.8 nM
2	IC50 = 2 nM
CP0234676 Compound Info	1-(4-(((6-amino-5-(4-phenoxyphenyl)pyrimidin-4-yl)amino)methyl)piperidin-1-yl)prop-2-en-1-one Show/Hide	C25H27N5O2	5
1	IC50 = 1.83 nM
2	IC50 = 5 nM
3	IC50 = 62 nM
4	IC50 = 8600 nM
5	Kd = 16 nM
CP0119549 Compound Info	US10005782, Compound 94 Show/Hide	C23H23N5O3	1
1	IC50 = 1.9 nM
CP0339333 Compound Info	US10005782, Compound 151 Show/Hide	C22H20FN5O2	1
1	IC50 = 1.9 nM
CP0455610 Compound Info	N-[3-[3-[(2-chloro-6-fluorophenyl)methylamino]-1H-1,2,4-triazol-5-yl]phenyl]prop-2-enamide Show/Hide	C18H15ClFN5O	1
1	IC50 = 1.91 nM
CP0075633 Compound Info	(E)-4-(dimethylamino)-N-[7-fluoro-4-(2-methylanilino)imidazo[1,5-a]quinoxalin-8-yl]-N-methylbut-2-enamide Show/Hide	C24H25FN6O	2
1	IC50 = 1.93 nM
2	IC50 = 3.31 nM
CP0781574 Compound Info	(S)-5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)-isoquinolin-3-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one Show/Hide	C18H17N5O3	1
1	IC50 < 1.995 nM
CP0072538 Compound Info	4-amino-8-(5-methyl-1H-indazol-6-yl)cinnoline-3-carboxamide Show/Hide	C17H14N6O	1
1	IC50 = 2 nM
CP0132679 Compound Info	US9233111, 62 Show/Hide	C28H34FN7O3	1
1	IC50 = 2 nM
CP0442933 Compound Info	US9233111, 16 Show/Hide	C31H33FN6O4	1
1	IC50 = 2 nM
CP0958076 Compound Info	(S)-2,3-Dimethyl-4-((1-propioloylpyrrolidin-3-yl)amino)-1H-indole-7-carboxamide Show/Hide	C18H20N4O2	1
1	IC50 = 2.4 nM
CP0543405 Compound Info	2-[3-(hydroxymethyl)-4-[8-[(5-methyl-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-2-yl)amino]imidazo[1,2-b]pyridazin-6-yl]pyridin-2-yl]-3,4,6,7,8,9-hexahydropyrazino[1,2-a]indol-1-one Show/Hide	C30H32N10O2	2
1	IC50 = 2.5 nM
2	IC50 = 3.2 nM
CP0205238 Compound Info	US10005782, Compound 50 Show/Hide	C27H21N5O3	1
1	IC50 = 2.7 nM
CP0205241 Compound Info	US10005782, Compound 22 Show/Hide	C25H27N5O4	1
1	IC50 = 2.7 nM
CP0110824 Compound Info	N-[4-amino-6-methylidene-5-(4-phenoxyphenyl)-7,8-dihydropyrimido[5,4-b]pyrrolizin-7-yl]prop-2-enamide Show/Hide	C25H21N5O2	1
1	IC50 = 2.8 nM
CP0086121 Compound Info	ACP-196 Show/Hide	C26H23N7O2	6
1	IC50 = 3 nM
2	IC50 = 3.1 nM
3	IC50 = 5.1 nM
4	IC50 = 19 nM
5	Kd = 2.6 nM
6	Kd = 21 nM
CP0321138 Compound Info	(E)-2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-3-(3-methyloxetan-3-yl)prop-2-enenitrile Show/Hide	C30H28FN7O3	1
1	IC50 = 3.1 nM
CP0163945 Compound Info	US10604504, Example 93 Show/Hide	C19H24N4O2	1
1	IC50 = 3.3 nM
CP0878824 Compound Info	(RS)-4-(3-Acrylamidopiperidin-1-yl)-2,3-dimethyl-1H-indole-7-carboxamide Show/Hide	C19H24N4O2	1
1	IC50 = 3.3 nM
CP0474172 Compound Info	US10005782, Compound 108 Show/Hide	C25H25N5O3	1
1	IC50 = 3.5 nM
CP0807542 Compound Info	(RS)-2,3-Dimethyl-4-(3-(vinylsulfonamido)pyrrolidin-1-yl)-1H-indole-7-carboxamide Show/Hide	C17H22N4O3S	1
1	IC50 = 3.5 nM
CP0092548 Compound Info	4-(8-amino-3-{(3R,6S)-6-methyl-1-[(3-methyloxetan-3-yl)carbonyl]piperidin-3-yl}imidazo[1,5-a]pyrazin-1-yl)-3-fluoro-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C29H27F4N7O2	1
1	IC50 = 4 nM
CP0534851 Compound Info	N-[3-[6-cyclohexyl-2-[3-(2-methoxyethoxy)anilino]-7-oxopteridin-8-yl]phenyl]prop-2-enamide Show/Hide	C30H32N6O4	1
1	IC50 = 4 nM
CP0234528 Compound Info	US10005782, Compound 161 Show/Hide	C23H20F3N5O2	1
1	IC50 = 4.2 nM
CP0361464 Compound Info	US10005782, Compound 149 Show/Hide	C23H20F3N5O3	1
1	IC50 = 4.2 nM
CP0688212 Compound Info	(RS)-4-(3-Acrylamidopyrrolidin-1-yl)-2,3-dimethyl-1H-indole-7-carboxamide Show/Hide	C18H22N4O2	1
1	IC50 = 4.2 nM
CP0132360 Compound Info	2-methyl-N-[2-[3-[[2-(prop-2-enoylamino)acetyl]amino]anilino]pyrimidin-5-yl]-5-[[3-(trifluoromethyl)benzoyl]amino]benzamide Show/Hide	C31H26F3N7O4	1
1	IC50 < 4.4 nM
CP0264919 Compound Info	US10005782, Compound 14 Show/Hide	C29H27N5O3	1
1	IC50 = 4.7 nM
CP0115886 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[6-[1-(morpholine-4-carbonyl)-3,6-dihydro-2H-pyridin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]isoquinolin-1-one Show/Hide	C35H33FN6O4	1
1	IC50 = 4.8 nM
CP0113747 Compound Info	2-methyl-N-[2-[3-(prop-2-enoylamino)anilino]pyrimidin-5-yl]-5-[[3-(trifluoromethyl)benzoyl]amino]benzamide Show/Hide	C29H23F3N6O3	1
1	IC50 = 5 nM
CP0689423 Compound Info	US9233111, 3 Show/Hide	C31H33FN6O2S	1
1	IC50 = 5 nM
CP0118988 Compound Info	4-[8-amino-1-(4-{[4- (trifluoromethyl) pyridin-2- yl]carbamoyl}phenyl) imidazo[1,5-a]pyrazin- 3- yl]bicyclo[2.2.2] octane-1-carboxylic acid Show/Hide	C28H25F3N6O3	1
1	IC50 = 5 nM
CP0413050 Compound Info	4-[8-amino-3-[(1R,3S)-3-(2-methyltetrazol-5-yl)cyclohexyl]imidazo[1,5-a]pyrazin-1-yl]-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C27H25F3N10O	1
1	IC50 = 5 nM
CP0150519 Compound Info	4-[8-amino-3-[(3R)-1-(2-methylpropanoyl)piperidin-3-yl]imidazo[1,5-a]pyrazin-1-yl]-3-fluoro-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C28H27F4N7O2	1
1	IC50 = 5 nM
CP0261533 Compound Info	4-[8-amino-3-[(2R,5S)-4-(cyclopropanecarbonyl)-5-methylmorpholin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-3-fluoro-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C28H25F4N7O3	1
1	IC50 = 5.3 nM
CP0244549 Compound Info	CHEMBL4081444 Show/Hide	C29H27F3N6O3	1
1	IC50 = 6 nM
CP0475905 Compound Info	4-[3-[(2R)-4-acetylmorpholin-2-yl]-8-aminoimidazo[1,5-a]pyrazin-1-yl]-3-fluoro-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C25H21F4N7O3	1
1	IC50 = 6 nM
CP0752388 Compound Info	(R)-2,3-Dimethyl-4-(3-propiolamidopyrrolidin-1-yl)-1H-indole-7-carboxamide Show/Hide	C18H20N4O2	1
1	IC50 = 6.5 nM
CP0271871 Compound Info	4-[4-[3-(6-cyclopropyl-8-fluoro-1-oxoisoquinolin-2-yl)-2-(hydroxymethyl)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-N,N-dimethyl-3,6-dihydro-2H-pyridine-1-carboxamide Show/Hide	C33H31FN6O3	1
1	IC50 = 7 nM
CP0180499 Compound Info	4-[8-amino-3-[(3R)-1-(1-methylcyclobutanecarbonyl)piperidin-3-yl]imidazo[1,5-a]pyrazin-1-yl]-3-fluoro-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C30H29F4N7O2	1
1	IC50 = 7 nM
CP0068199 Compound Info	9-(1-methylpyrazol-4-yl)-1-(1-prop-2-enoyl-2,3-dihydroindol-6-yl)benzo[h][1,6]naphthyridin-2-one Show/Hide	C27H21N5O2	1
1	IC50 = 7 nM
CP0092554 Compound Info	(1S,3R)-3-[8-amino-1- (4-{[4- (trifluoromethyl) pyridin-2- yl]carbamoyl}phenyl) imidazo[1,5-a]pyrazin- 3-yl]-1,3- dimethylcyclopentane carboxylic acid Show/Hide	C27H25F3N6O3	1
1	IC50 = 8 nM
CP0189278 Compound Info	(R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl) piperidin-3-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(4-(trifluoromethyl)pyridin-2-yl)benzamide Show/Hide	C29H28F3N7O3	1
1	IC50 = 8 nM
CP0059735 Compound Info	4-tert-butyl-N-[2-methyl-3-[6-[4-(morpholine-4-carbonyl)anilino]-7H-purin-2-yl]phenyl]benzamide Show/Hide	C34H35N7O3	1
1	IC50 = 8 nM
CP0839280 Compound Info	(R)-4-((1-Acryloylpyrrolidin-3-yl)amino)-2,3-dimethyl-1H-indole-7-carboxamide Show/Hide	C18H22N4O2	1
1	IC50 = 8.4 nM
CP0438691 Compound Info	methyl 1-[2-[4-[[5-chloro-4-[3-(prop-2-enoylamino)anilino]pyrimidin-2-yl]amino]phenoxy]acetyl]pyrrolidine-2-carboxylate Show/Hide	C27H27ClN6O5	1
1	IC50 = 8.7 nM
CP0304840 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-[4-(1-methylazetidin-3-yl)piperazin-1-yl]pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]isoquinolin-1-one Show/Hide	C38H40FN7O3	1
1	IC50 = 9 nM
CP0114109 Compound Info	CHEMBL4068131 Show/Hide	C27H23F3N6O3	1
1	IC50 = 9 nM
CP0205240 Compound Info	US10005782, Compound 99 Show/Hide	C28H25N5O3	1
1	IC50 = 9.5 nM
CP0284384 Compound Info	3-(1-propan-2-yloxyisoquinolin-3-yl)-1,4-dihydro-1,2,4-triazol-5-one Show/Hide	C14H14N4O2	1
1	IC50 = 10 nM
CP0244548 Compound Info	(1R,3R,5S,6r)-3-[8- amino-1-(4-{[4- (trifluoromethyl) pyridin-2- yl]carbamoyl}phenyl) imidazo[1,5-a]pyrazin- 3- yl]bicyclo[3.1.0] hexane-6-carboxylic acid Show/Hide	C26H21F3N6O3	1
1	IC50 = 11 nM
CP0080849 Compound Info	10-[3-(hydroxymethyl)-4-[1-methyl-5-[[5-[(2S)-2-methyl-4-(oxetan-3-yl)piperazin-1-yl]pyridin-2-yl]amino]-6-oxopyridin-3-yl]pyridin-2-yl]-4,4-dimethyl-1,10-diazatricyclo[6.4.0.02,6]dodeca-2(6),7-dien-9-one Show/Hide	C37H44N8O4	3
1	IC50 = 11 nM
2	Ki = 0.9 nM
3	Ki = 1.6 nM
CP0313624 Compound Info	4-(8-amino-3-{(3R)-1-[(3-methyloxetan-3-yl)carbonyl]piperidin-3-yl}imidazo[1,5-a]pyrazin-1-yl)-N-(4-chloropyridin-2-yl)-3-fluorobenzamide Show/Hide	C26H23F4N7O2	1
1	IC50 = 11 nM
CP0072649 Compound Info	4-(8-amino-3-{(3R)-1-[(3-methyloxetan-3-yl)carbonyl]azepan-3-yl}imidazo[1,5-a]pyrazin-1-yl)-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C27H25F4N7O3	1
1	IC50 = 13 nM
CP0072650 Compound Info	4-[8-amino-3-[(2R)-4-(oxan-4-yl)morpholin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-3-fluoro-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C28H27F4N7O3	1
1	IC50 = 13 nM
CP0209157 Compound Info	N-[2-(3-aminoanilino)pyrimidin-5-yl]-2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]benzamide Show/Hide	C26H21F3N6O2	1
1	IC50 = 14 nM
CP0063953 Compound Info	US10005782, Compound 130 Show/Hide	C25H19N5O3	1
1	IC50 = 14 nM
CP0525586 Compound Info	US10005782, Compound 66 Show/Hide	C22H17N5O2	1
1	IC50 = 14 nM
CP0072648 Compound Info	4-{8-amino-3-[(2R)-4-oxetan-3-ylmorpholin-2-yl]imidazo[1,5-a]pyrazin-1-yl}-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C26H23F4N7O4	1
1	IC50 = 14 nM
CP0239951 Compound Info	US10106559, Comparative Example 75 Show/Hide	C31H26N4O3	1
1	IC50 = 14 nM
CP0386753 Compound Info	2-[3-[6-(1-acetyl-3,6-dihydro-2H-pyridin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-2-(hydroxymethyl)phenyl]-6-cyclopropyl-8-fluoroisoquinolin-1-one Show/Hide	C32H28FN5O3	1
1	IC50 = 15.3 nM
CP0068442 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[6-(1-methylsulfonyl-3,6-dihydro-2H-pyridin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]isoquinolin-1-one Show/Hide	C31H28FN5O4S	1
1	IC50 = 15.8 nM
CP0042946 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-[4-(oxetan-3-yl)piperazin-1-yl]pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]isoquinolin-1-one Show/Hide	C37H37FN6O4	1
1	IC50 = 16 nM
CP0320927 Compound Info	4-[4-[3-(6-cyclopropyl-8-fluoro-1-oxoisoquinolin-2-yl)-2-(hydroxymethyl)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-N,N-dimethyl-3,6-dihydro-2H-pyridine-1-sulfonamide Show/Hide	C32H31FN6O4S	1
1	IC50 = 16.5 nM
CP0201176 Compound Info	CHEMBL4079697 Show/Hide	C28H27F3N6O3	1
1	IC50 = 17 nM
CP0250873 Compound Info	4-[8-amino-3-[(1R,3S)-3-carbamoylcyclohexyl]imidazo[1,5-a]pyrazin-1-yl]-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C26H24F3N7O2	1
1	IC50 = 17 nM
CP0562980 Compound Info	4-[8-amino-3-[(1R,3S)-3-(1H-1,2,4-triazol-5-yl)cyclohexyl]imidazo[1,5-a]pyrazin-1-yl]-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C27H24F3N9O	1
1	IC50 = 17 nM
CP0170723 Compound Info	4-[4-[3-(6-cyclopropyl-8-fluoro-1-oxoisoquinolin-2-yl)-2-(hydroxymethyl)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-N,N-dimethylbenzamide Show/Hide	C34H28FN5O3	1
1	IC50 = 17.8 nM
CP0056961 Compound Info	(1S,3R)-3-[8-amino-1-[4-[[4-(trifluoromethyl)pyridin-2-yl]carbamoyl]phenyl]imidazo[1,5-a]pyrazin-3-yl]-1,3-dimethylcyclohexane-1-carboxylic acid Show/Hide	C28H27F3N6O3	1
1	IC50 = 18 nM
CP0320926 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[6-[4-(morpholine-4-carbonyl)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]isoquinolin-1-one Show/Hide	C36H30FN5O4	1
1	IC50 = 18.2 nM
CP0546193 Compound Info	3-[1-(propan-2-ylamino)isoquinolin-3-yl]-1,4-dihydro-1,2,4-triazol-5-one Show/Hide	C14H15N5O	1
1	IC50 = 19.95 nM
CP0529516 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]isoquinolin-1-one Show/Hide	C38H38FN5O4	1
1	IC50 = 20 nM
CP0114110 Compound Info	(1R,3R)-3-[8-amino-1-[4-[[4-(trifluoromethyl)pyridin-2-yl]carbamoyl]phenyl]imidazo[1,5-a]pyrazin-3-yl]-3-methyl-1-propan-2-ylcyclopentane-1-carboxylic acid Show/Hide	C29H29F3N6O3	1
1	IC50 = 20 nM
CP0244546 Compound Info	4-[8-amino-3-[(1R,3S)-3-(1-methyltetrazol-5-yl)cyclohexyl]imidazo[1,5-a]pyrazin-1-yl]-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C27H25F3N10O	1
1	IC50 = 21 nM
CP0322301 Compound Info	N-[3-[[4-[4-(piperidine-1-carbonyl)anilino]-1,3,5-triazin-2-yl]amino]phenyl]prop-2-enamide Show/Hide	C24H25N7O2	1
1	IC50 = 21 nM
CP0487784 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[6-(1-methylpyrazol-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]isoquinolin-1-one Show/Hide	C29H23FN6O2	1
1	IC50 = 21.3 nM
CP0081924 Compound Info	(1R,2R,5R)-5-[8- amino-1-(4-{[4- (trifluoromethyl) pyridin-2- yl]carbamoyl}phenyl) imidazo[1,5-a]pyrazin- 3-yl]-2-(1- methylethyl) cyclohexane- carboxylic acid Show/Hide	C29H29F3N6O3	1
1	IC50 = 22 nM
CP0564914 Compound Info	US9233111, 24 Show/Hide	C29H29FN4OS	1
1	IC50 = 23 nM
CP0196920 Compound Info	4-[8-amino-1-(2- ethoxy-4-{[4- (trifluoromethyl) pyridin-2- yl]carbamoyl}phenyl) imidazo[1,5-a]pyrazin- 3- yl]bicyclo[2.2.2] octane-1-carboxylic acid Show/Hide	C30H29F3N6O4	1
1	IC50 = 24 nM
CP0068443 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[6-[1-(oxetan-3-yl)-3,6-dihydro-2H-pyridin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]isoquinolin-1-one Show/Hide	C33H30FN5O3	1
1	IC50 = 24.8 nM
CP0573587 Compound Info	3-(1-propoxyisoquinolin-3-yl)-1,4-dihydro-1,2,4-triazol-5-one Show/Hide	C14H14N4O2	1
1	IC50 = 25.12 nM
CP0231326 Compound Info	4-[4-[3-(6-cyclopropyl-8-fluoro-1-oxoisoquinolin-2-yl)-2-(hydroxymethyl)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-N-methyl-3,6-dihydro-2H-pyridine-1-carboxamide Show/Hide	C32H29FN6O3	1
1	IC50 = 25.2 nM
CP0483603 Compound Info	(1S,3R)-3-[8-amino-1- (4-{[4- (trifluoromethyl) pyridin-2- yl]carbamoyl}phenyl) imidazo[1,5-a]pyrazin- 3-yl]-1- methylcyclohexane- carboxylic acid Show/Hide	C27H25F3N6O3	1
1	IC50 = 26 nM
CP0108285 Compound Info	4-[8-amino-3-[(2R)-4-(2-methylpropanoyl)morpholin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-3-fluoro-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C27H25F4N7O3	1
1	IC50 = 26 nM
CP0561590 Compound Info	US9233111, 38 Show/Hide	C31H32FN5O3	1
1	IC50 = 27 nM
CP0244547 Compound Info	(1S,3R)-3-[8-amino-1- (4-{[4- (trifluoromethyl) pyridin-2- yl]carbamoyl}phenyl) imidazo[1,5-a]pyrazin- 3-yl]-1-(1- methylethyl) cyclopentane carboxylic acid Show/Hide	C28H27F3N6O3	1
1	IC50 = 27 nM
CP0474077 Compound Info	2-[3-[5-[[5-[4-(cyclopropanecarbonyl)piperazin-1-yl]pyridin-2-yl]amino]-1-methyl-6-oxopyridin-3-yl]-2-(hydroxymethyl)phenyl]-6-cyclopropyl-8-fluoroisoquinolin-1-one Show/Hide	C38H37FN6O4	1
1	IC50 = 28 nM
CP0713343 Compound Info	(RS)-2,3-Dimethyl-4-((1-propioloylpiperidin-3-yl)amino)-1H-indole-7-carboxamide Show/Hide	C19H22N4O2	1
1	IC50 = 29 nM
CP0386752 Compound Info	6-cyclopropyl-2-[3-[6-[4-[(dimethylamino)methyl]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-2-(hydroxymethyl)phenyl]-8-fluoroisoquinolin-1-one Show/Hide	C34H30FN5O2	1
1	IC50 = 31.6 nM
CP0968712 Compound Info	(R)-5-(1-((1-acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one Show/Hide	C18H17N5O3	1
1	IC50 = 31.62 nM
CP0147799 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[6-(1,2,3,6-tetrahydropyridin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]isoquinolin-1-one Show/Hide	C30H26FN5O2	1
1	IC50 = 32.5 nM
CP0715572 Compound Info	US9447106, 117 Show/Hide	C25H23N5O3	1
1	IC50 = 34 nM
CP0313625 Compound Info	4-[8-amino-3-[(2R)-4-(1-methylcyclobutanecarbonyl)morpholin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-3-fluoro-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C29H27F4N7O3	1
1	IC50 = 35 nM
CP0304838 Compound Info	6-cyclopropyl-2-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]isoquinolin-1-one Show/Hide	C35H36N6O3	1
1	IC50 = 37 nM
CP0196917 Compound Info	4-[8-amino-3-[(1R,3S)-3-(2-oxo-3H-1,3,4-oxadiazol-5-yl)cyclohexyl]imidazo[1,5-a]pyrazin-1-yl]-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C27H23F3N8O3	1
1	IC50 = 37 nM
CP0189973 Compound Info	4-[8-amino-3-[(3R)-1-(3-methyloxetane-3-carbonyl)pyrrolidin-3-yl]imidazo[1,5-a]pyrazin-1-yl]-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C28H26F3N7O3	1
1	IC50 = 37 nM
CP0379329 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[6-(1H-pyrazol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]isoquinolin-1-one Show/Hide	C28H21FN6O2	1
1	IC50 = 38.8 nM
CP0203204 Compound Info	N-[3-[[2-(3-aminoanilino)pyrimidin-5-yl]carbamoyl]-4-methylphenyl]naphthalene-2-carboxamide Show/Hide	C29H24N6O2	1
1	IC50 = 39 nM
CP0459751 Compound Info	US10005782, Compound 109 Show/Hide	C25H27N5O3	1
1	IC50 = 41 nM
CP0231346 Compound Info	2-[3-[6-(4-acetylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-2-(hydroxymethyl)phenyl]-6-cyclopropyl-8-fluoroisoquinolin-1-one Show/Hide	C33H25FN4O3	1
1	IC50 = 41.7 nM
CP0320928 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[6-(1-pyrimidin-2-yl-3,6-dihydro-2H-pyridin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]isoquinolin-1-one Show/Hide	C34H28FN7O2	1
1	IC50 = 45.3 nM
CP0273436 Compound Info	(Z)-2-[(2R)-2-[[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]methyl]pyrrolidine-1-carbonyl]-3-cyclopropylprop-2-enenitrile Show/Hide	C29H26FN7O2	1
1	IC50 = 46 nM
CP0231883 Compound Info	4-{8-amino-3-[(2R)-4-(3-methoxypropanoyl)morpholin-2-yl]imidazo[1,5-a]pyrazin-1-yl}-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C28H26F3N7O4	1
1	IC50 = 48 nM
CP0196918 Compound Info	4-(8-amino-1-(2- fluoro-4-((4- (trifluoromethyl) pyridin-2- yl)carbamoyl)phenyl) imidazo[1,5-a]pyrazin- 3-yl)cubane-1- carboxylic acid Show/Hide	C28H18F4N6O3	1
1	IC50 = 49 nM
CP0170254 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[6-[4-(piperidine-1-carbonyl)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]isoquinolin-1-one Show/Hide	C37H32FN5O3	1
1	IC50 = 50.8 nM
CP0170256 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[6-(1-methyl-3,6-dihydro-2H-pyridin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]isoquinolin-1-one Show/Hide	C31H28FN5O2	1
1	IC50 = 57.1 nM
CP0319439 Compound Info	4-[8-amino-3-[(2R)-4-(3-methoxypropanoyl)morpholin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C27H26F3N7O4	1
1	IC50 = 58 nM
CP0089684 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[6-(4-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]isoquinolin-1-one Show/Hide	C32H25FN4O3	1
1	IC50 = 58.3 nM
CP0852081 Compound Info	(RS)-4-((1-Acryloylpiperidin-3-yl)amino)-2,3-dimethyl-1H-indole-7-carboxamide Show/Hide	C19H24N4O2	1
1	IC50 = 59 nM
CP0081927 Compound Info	(1S,3R)-3-[8-amino-1- (4-{[4- (trifluoromethyl) pyridin-2- yl]carbamoyl}phenyl) imidazo[1,5-a]pyrazin- 3-yl]-1- methylcyclopentane- carboxylic acid Show/Hide	C26H23F3N6O3	1
1	IC50 = 62 nM
CP0231324 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[6-[4-(morpholin-4-ylmethyl)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]isoquinolin-1-one Show/Hide	C36H32FN5O3	1
1	IC50 = 63.6 nM
CP0132601 Compound Info	4-[8-amino-3-[(3R)-1-(oxan-4-yl)piperidin-3-yl]imidazo[1,5-a]pyrazin-1-yl]-3-fluoro-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C29H29F4N7O2	1
1	IC50 = 65 nM
CP0323446 Compound Info	3-[8-amino-1-(4-{[4- (trifluoromethyl) pyridin-2- yl]carbamoyl}phenyl) imidazo[1,5-a]pyrazin- 3- yl]bicyclo[1.1.1] pentane-1-carboxylic acid Show/Hide	C25H19F3N6O3	1
1	IC50 = 67 nM
CP0258896 Compound Info	6-cyclopropyl-2-[3-[6-(3,6-dihydro-2H-thiopyran-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-2-(hydroxymethyl)phenyl]-8-fluoroisoquinolin-1-one Show/Hide	C30H25FN4O2S	1
1	IC50 = 67.1 nM
CP0170724 Compound Info	3-[4-[3-(6-cyclopropyl-8-fluoro-1-oxoisoquinolin-2-yl)-2-(hydroxymethyl)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-N,N-dimethylbenzamide Show/Hide	C34H28FN5O3	1
1	IC50 = 69 nM
CP0574996 Compound Info	(E)-2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-morpholin-4-ylpent-2-enenitrile Show/Hide	C33H35FN8O3	1
1	IC50 = 69 nM
CP0273438 Compound Info	(Z)-2-[(2R)-2-[[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]methyl]pyrrolidine-1-carbonyl]-4-methyl-4-morpholin-4-ylpent-2-enenitrile Show/Hide	C33H35FN8O3	1
1	IC50 = 72 nM
CP0170252 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[6-(4-hydroxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]isoquinolin-1-one Show/Hide	C31H23FN4O3	1
1	IC50 = 73.9 nM
CP0323445 Compound Info	CHEMBL4097968 Show/Hide	C26H23F3N6O3	1
1	IC50 = 77 nM
CP0334402 Compound Info	2-[3-[6-(cyclohexen-1-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-2-(hydroxymethyl)phenyl]-6-cyclopropyl-8-fluoroisoquinolin-1-one Show/Hide	C31H27FN4O2	1
1	IC50 = 77.8 nM
CP0319444 Compound Info	4-[8-amino-3-[1-(3-methyloxetane-3-carbonyl)piperidin-4-yl]imidazo[1,5-a]pyrazin-1-yl]-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C29H28F3N7O3	1
1	IC50 = 80 nM
CP0334401 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-(6-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]isoquinolin-1-one Show/Hide	C31H23FN4O2	1
1	IC50 = 90.3 nM
CP0114115 Compound Info	US10087188, Example 1 Show/Hide	C26H23F3N6O3	1
1	IC50 = 98 nM
CP0570423 Compound Info	3-[1-(ethylamino)isoquinolin-3-yl]-1,4-dihydro-1,2,4-triazol-5-one Show/Hide	C13H13N5O	1
1	IC50 = 100 nM
CP0115883 Compound Info	2-[3-[6-(5-acetylthiophen-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-2-(hydroxymethyl)phenyl]-6-cyclopropyl-8-fluoroisoquinolin-1-one Show/Hide	C31H23FN4O3S	1
1	IC50 = 118.8 nM
CP0032229 Compound Info	2-(dimethylamino)-N-[4-[8-(6-methoxypyridin-3-yl)-2-oxo-[1]benzofuro[3,2-b]pyridin-1-yl]phenyl]acetamide Show/Hide	C27H24N4O4	1
1	IC50 = 119 nM
CP0114111 Compound Info	(1S,3R)-3-[8-amino-1- (4-{[4- (trifluoromethyl) pyridin-2- yl]carbamoyl}phenyl) imidazo[1,5-a]pyrazin- 3-yl]-1-(1- methylethyl) cyclohexane- carboxylic acid Show/Hide	C29H29F3N6O3	1
1	IC50 = 128 nM
CP0355611 Compound Info	US10087188, Example 13 Show/Hide	C25H21F3N6O3	1
1	IC50 = 132 nM
CP0170253 Compound Info	2-[3-[6-(3-aminophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-2-(hydroxymethyl)phenyl]-6-cyclopropyl-8-fluoroisoquinolin-1-one Show/Hide	C31H24FN5O2	1
1	IC50 = 135.5 nM
CP0956168 Compound Info	(R)-N-(1-Acryloylpyrrolidin-3-yl)-5-(*S)-(2-methyl-4-phenoxyphenyl)-4-oxo-4,5-dihydro-3H-1-thia-3,5,8-triazaacenaphthylene-2-carboxamide Show/Hide	C29H25N5O4S	1
1	IC50 = 142 nM
CP0168512 Compound Info	US10005782, Compound 48 Show/Hide	C27H21N5O3	1
1	IC50 = 150 nM
CP0032295 Compound Info	N-[4-[8-(6-methoxypyridin-3-yl)-2-oxo-[1]benzofuro[3,2-b]pyridin-1-yl]phenyl]-2-(4-methylpiperazin-1-yl)acetamide Show/Hide	C30H29N5O4	1
1	IC50 = 153 nM
CP0560337 Compound Info	4-[8-amino-3-[1-(3-methyloxetane-3-carbonyl)azetidin-3-yl]imidazo[1,5-a]pyrazin-1-yl]-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C27H24F3N7O3	1
1	IC50 = 167 nM
CP0052934 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[6-(6-methoxypyridin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]isoquinolin-1-one Show/Hide	C31H24FN5O3	1
1	IC50 = 197.4 nM
CP0319723 Compound Info	US10005782, Compound 5 Show/Hide	C25H23N5O2	1
1	IC50 = 200 nM
CP0304835 Compound Info	6-cyclopropyl-8-fluoro-2-[2-methyl-3-[1-methyl-5-[[5-[4-(oxetan-3-yl)piperazin-1-yl]pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]isoquinolin-1-one Show/Hide	C37H37FN6O3	1
1	IC50 = 203 nM
CP0367258 Compound Info	6-cyclopropyl-2-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]-2,7-naphthyridin-1-one Show/Hide	C34H35N7O3	1
1	IC50 = 255 nM
CP0057678 Compound Info	6-cyclopropyl-8-fluoro-2-[2-methyl-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]isoquinolin-1-one Show/Hide	C35H35FN6O2	1
1	IC50 = 365 nM
CP0322784 Compound Info	N-[3-(8-anilinoimidazo[1,2-a]pyrazin-6-yl)phenyl]-4-tert-butylbenzamide Show/Hide	C29H27N5O	1
1	IC50 = 400 nM
CP0057680 Compound Info	6-(dimethylamino)-2-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]-2,7-naphthyridin-1-one Show/Hide	C33H36N8O3	1
1	IC50 = 431 nM
CP0367257 Compound Info	6-cyclopropyl-8-fluoro-2-[3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]isoquinolin-1-one Show/Hide	C34H33FN6O2	1
1	IC50 = 503 nM
CP0118989 Compound Info	4-[8-amino-1-[4-[[4-(trifluoromethyl)pyridin-2-yl]carbamoyl]phenyl]imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclohexane-1-carboxylic acid Show/Hide	C27H25F3N6O3	1
1	IC50 = 546 nM
CP0568055 Compound Info	7-[(3S)-4-methyl-6-(2-methylpropyl)-2,3-dihydropyridin-3-yl]-6-oxo-N-[(1R,2S)-2-(prop-2-enoylamino)cyclopentyl]-2-thia-5,7,11-triazatricyclo[6.3.1.04,12]dodeca-1(11),3,8(12),9-tetraene-3-carboxamide Show/Hide	C27H32N6O3S	1
1	IC50 = 558 nM
CP0042945 Compound Info	2-cyclopropyl-6-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]-1,6-naphthyridin-5-one Show/Hide	C34H35N7O3	1
1	IC50 = 564 nM
CP0052935 Compound Info	4-[4-[3-(6-cyclopropyl-8-fluoro-1-oxoisoquinolin-2-yl)-2-(hydroxymethyl)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-N,N-dimethylpiperidine-1-carboxamide Show/Hide	C33H33FN6O3	1
1	IC50 = 574 nM
CP0114107 Compound Info	4-[8-amino-3-[(1R,3S)-3-(methylsulfonylcarbamoyl)cyclohexyl]imidazo[1,5-a]pyrazin-1-yl]-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C27H26F3N7O4S	1
1	IC50 = 648 nM
CP0865423 Compound Info	rac-1-(3-(1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-3-yl)phenyl)-3-phenylurea Show/Hide	C24H24N6O	1
1	IC50 = 800 nM
CP0304836 Compound Info	N-[5-[3-(6-cyclopropyl-8-fluoro-1-oxoisoquinolin-2-yl)-2-(hydroxymethyl)phenyl]-1-methyl-2-oxopyridin-3-yl]-4-(4-methylpiperazin-1-yl)benzamide Show/Hide	C37H36FN5O4	1
1	IC50 = 818 nM
CP0525587 Compound Info	US10005782, Compound 8 Show/Hide	C28H21N5O3	1
1	IC50 = 860 nM
CP0550420 Compound Info	4-tert-butyl-N-[2-methyl-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]benzamide Show/Hide	C34H40N6O2	1
1	IC50 = 875 nM
CP0196916 Compound Info	4-[8-amino-3-[(1R,3S)-3-(5-oxo-4H-1,2,4-oxadiazol-3-yl)cyclohexyl]imidazo[1,5-a]pyrazin-1-yl]-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C27H23F3N8O3	1
1	IC50 = 979 nM
CP0474173 Compound Info	US10005782, Compound 13 Show/Hide	C26H25N5O2	1
1	IC50 = 1000 nM
CP0207024 Compound Info	4-[8-amino-3-(morpholin-4-ylmethyl)imidazo[1,5-a]pyrazin-1-yl]-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C24H22F3N7O2	1
1	IC50 = 1225 nM
CP0250874 Compound Info	US10087188, Example 158 Show/Hide	C26H23F3N6O3	1
1	IC50 = 1237 nM
CP0258895 Compound Info	4-[3-(6-cyclopropyl-8-fluoro-1-oxoisoquinolin-2-yl)-2-(hydroxymethyl)phenyl]-N,N-dimethyl-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide Show/Hide	C28H24FN5O3	1
1	IC50 = 1357 nM
CP0334400 Compound Info	6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]isoquinolin-1-one Show/Hide	C25H19FN4O2	1
1	IC50 = 1568 nM
CP0196915 Compound Info	4-[8-amino-3-[(1R,3S)-3-(2H-tetrazol-5-yl)cyclohexyl]imidazo[1,5-a]pyrazin-1-yl]-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide Show/Hide	C26H23F3N10O	1
1	IC50 = 1587 nM
CP0204006 Compound Info	4-aminocinnoline-3-carboxamide Show/Hide	C9H8N4O	1
1	IC50 = 3162.28 nM
CP0068444 Compound Info	4-[4-[3-(6-cyclopropyl-8-fluoro-1-oxoisoquinolin-2-yl)-2-(hydroxymethyl)phenyl]-7-methylpyrrolo[2,3-d]pyrimidin-6-yl]-N,N-dimethyl-3,6-dihydro-2H-pyridine-1-carboxamide Show/Hide	C34H33FN6O3	1
1	IC50 > 5000 nM
CP0243780 Compound Info	3-amino-2-[(2S)-1-prop-2-enoylpiperidin-2-yl]-5-[4-[[4-(trifluoromethyl)pyridin-2-yl]carbamoyl]phenyl]imidazole-4-carboxamide Show/Hide	C25H24F3N7O3	1
1	IC50 > 10000 nM

Clinical Information about the Protein

Target 1 ( Tyrosine-protein kinase BTK (ATK) )

Target Type	Successful Target
Disease	10 Target-related Diseases				10
1	Mantle cell lymphoma [ICD-11: 2A85.5]
2	Non-hodgkin lymphoma [ICD-11: 2B33.5]
3	Multiple sclerosis [ICD-11: 8A40]
4	Hematologic tumour [ICD-11: 2B33.Y]
5	Rheumatoid arthritis [ICD-11: FA20]
6	Chronic lymphocytic leukaemia [ICD-11: 2A82.0]
7	B-cell lymphoma [ICD-11: 2A86]
8	Pemphigus vulgaris [ICD-11: EB40]
9	Atopic dermatitis [ICD-11: EA80]
10	Autoimmune diabetes [ICD-11: 5A10]
Approved Drug(s)	4 Approved Drugs				4
1	Acalabrutinib	Drug Info	Approved	Mantle cell lymphoma
2	Ibrutinib	Drug Info	Approved	Mantle cell lymphoma
3	Pirtobrutinib	Drug Info	Approved	Non-hodgkin lymphoma
4	Zanubrutinib	Drug Info	Approved	Mantle cell lymphoma
Clinical Trial Drug(s)	14 Clinical Trial Drugs				14
1	Tolebrutinib	Drug Info	Phase 3	Multiple sclerosis
2	ARQ 531	Drug Info	Phase 2	Hematologic tumour
3	BMS-986142	Drug Info	Phase 2	Rheumatoid arthritis
4	Branebrutinib	Drug Info	Phase 2	Rheumatoid arthritis
5	CC-292	Drug Info	Phase 2	Chronic lymphocytic leukaemia
6	GS-4059	Drug Info	Phase 2	B-cell lymphoma
7	ICP-022	Drug Info	Phase 3	Chronic lymphocytic leukaemia
8	M2951	Drug Info	Phase 2	Multiple sclerosis
9	PRN1008	Drug Info	Phase 2	Pemphigus vulgaris
10	SAR 444727	Drug Info	Phase 2	Atopic dermatitis
11	Vecabrutinib	Drug Info	Phase 1/2	B-cell lymphoma
12	BIIB091	Drug Info	Phase 1	Multiple sclerosis
13	GDC-0853	Drug Info	Phase 3	Multiple sclerosis
14	HM71224	Drug Info	Phase 1	Rheumatoid arthritis
Discontinued Drug(s)	1 Discontinued Drug				1
1	GDC-0834	Drug Info	Terminated	Rheumatoid arthritis
Investigative Drug(s)	1 Investigative Drug				1
1	CGI-1316	Drug Info	Investigative	Autoimmune diabetes

Target 2 ( HUMAN bruton tyrosine kinase (BTK) )

Target Type	Unknown Type Target
Disease	1 Target-related Disease				1
1	leukaemia [ICD-11: 2A60-2B33]
Clinical Trial Drug(s)	1 Clinical Trial Drug				1
1	Acalabrutinib	Drug Info	Approved	leukaemia

Similar Protein(s) and Bioactivity Statistics

90% Identity

Protein ID	Protein Name	Protein Organism
PT03989	Tyrosine-protein kinase BTK	Mus musculus, Mouse	Protein Info

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