Protein Information

General Information of the Protein

Protein ID	PT01659
Protein Name	Tyrosine-protein kinase JAK1
Secondarily Protein Name	Janus kinase 1
Gene Name	JAK1
Secondarily Gene Name	JAK1A JAK1B
Sequence	MQYLNIKEDCNAMAFCAKMRSSKKTEVNLEAPEPGVEVIFYLSDREPLRLGSGEYTAEELCIRAAQACRISPLCHNLFALYDENTKLWYAPNRTITVDDKMSLRLHYRMRFYFTNWHGTNDNEQSVWRHSPKKQKNGYEKKKIPDATPLLDASSLEYLFAQGQYDLVKCLAPIRDPKTEQDGHDIENECLGMAVLAISHYAMMKKMQLPELPKDISYKRYIPETLNKSIRQRNLLTRMRINNVFKDFLKEFNNKTICDSSVSTHDLKVKYLATLETLTKHYGAEIFETSMLLISSENEMNWFHSNDGGNVLYYEVMVTGNLGIQWRHKPNVVSVEKEKNKLKRKKLENKHKKDEEKNKIREEWNNFSYFPEITHIVIKESVVSINKQDNKKMELKLSSHEEALSFVSLVDGYFRLTADAHHYLCTDVAPPLIVHNIQNGCHGPICTEYAINKLRQEGSEEGMYVLRWSCTDFDNILMTVTCFEKSEQVQGAQKQFKNFQIEVQKGRYSLHGSDRSFPSLGDLMSHLKKQILRTDNISFMLKRCCQPKPREISNLLVATKKAQEWQPVYPMSQLSFDRILKKDLVQGEHLGRGTRTHIYSGTLMDYKDDEGTSEEKKIKVILKVLDPSHRDISLAFFEAASMMRQVSHKHIVYLYGVCVRDVENIMVEEFVEGGPLDLFMHRKSDVLTTPWKFKVAKQLASALSYLEDKDLVHGNVCTKNLLLAREGIDSECGPFIKLSDPGIPITVLSRQECIERIPWIAPECVEDSKNLSVAADKWSFGTTLWEICYNGEIPLKDKTLIEKERFYESRCRPVTPSCKELADLMTRCMNYDPNQRPFFRAIMRDINKLEEQNPDIVSEKKPATEVDPTHFEKRFLKRIRDLGEGHFGKVELCRYDPEGDNTGEQVAVKSLKPESGGNHIADLKKEIEILRNLYHENIVKYKGICTEDGGNGIKLIMEFLPSGSLKEYLPKNKNKINLKQQLKYAVQICKGMDYLGSRQYVHRDLAARNVLVESEHQVKIGDFGLTKAIETDKEYYTVKDDRDSPVFWYAPECLMQSKFYIASDVWSFGVTLHELLTYCDSDSSPMALFLKMIGPTHGQMTVTRLVNTLKEGKRLPCPPNCPDEVYQLMRKCWEFQPSNRTSFQNLIEGFEALLK Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme > Kinase > Protein Kinase > TK protein kinase group > Tyrosine protein kinase JakB family
Function	Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway (PubMed:8232552, PubMed:7615558, PubMed:28111307, PubMed:32750333, PubMed:16239216). Kinase partner for the interleukin (IL)-2 receptor (PubMed:11909529) as well as interleukin (IL)-10 receptor (PubMed:12133952). Kinase partner for the type I interferon receptor IFNAR2 (PubMed:8232552, PubMed:7615558, PubMed:28111307, PubMed:32750333, PubMed:16239216). In response to interferon-binding to IFNAR1-IFNAR2 heterodimer, phosphorylates and activates its binding partner IFNAR2, creating docking sites for STAT proteins (PubMed:7759950). Directly phosphorylates STAT proteins but also activates STAT signaling through the transactivation of other JAK kinases associated with signaling receptors (PubMed:8232552, PubMed:16239216, PubMed:32750333). Show/Hide
Uniprot ID	Primary ID: P23458 Secondarily ID: Q59GQ2 Q9UD26 Show/Hide
Ensembl ID	ENSG00000162434
HGNC ID	HGNC:6190
Subcellular Location	Endomembrane system

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: CL000077 , Ba/F3

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0807417 Compound Info	4-(((2S,4S)-1-(4-Chlorobenzyl)-2-methylpiperidin-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide Show/Hide	C22H26ClN5O	1
1	GI50 = 6.4 nM Bioactivity Info	TI LI LO TS
CP0002393 Compound Info	3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile Show/Hide	C16H20N6O	2
1	GI50 = 95.3 nM Bioactivity Info	TI LI LO TS
2	IC50 = 26 nM Bioactivity Info	TI LI LO TS
CP0957903 Compound Info	5-(6-acetamidopyrimidin-4-yloxy)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)indoline-1-carboxamide Show/Hide	C28H30F3N7O3	1
1	GI50 = 129 nM Bioactivity Info	TI LI LO TS
CP0807416 Compound Info	4-((cis-3-Fluoro-1-(3-methoxybenzyl)piperidin-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide Show/Hide	C22H26FN5O2	1
1	GI50 = 214 nM Bioactivity Info	TI LI LO TS
CP0952685 Compound Info	4-((trans-1-(3-Chlorobenzyl)-2-methylpiperidin-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide Show/Hide	C22H26ClN5O	1
1	GI50 = 232 nM Bioactivity Info	TI LI LO TS
CP0952760 Compound Info	4-((1-(3-Chlorobenzyl)azepan-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide Show/Hide	C22H26ClN5O	1
1	GI50 = 476 nM Bioactivity Info	TI LI LO TS
CP0008628 Compound Info	US10112907, Example 00033 Show/Hide	C21H23N5O3S	1
1	GI50 = 798 nM Bioactivity Info	TI LI LO TS
CP0807413 Compound Info	4-((8-(4-Chlorobenzyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide Show/Hide	C23H26ClN5O	1
1	GI50 = 1795 nM Bioactivity Info	TI LI LO TS
CP0065873 Compound Info	1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]-2-(dimethylamino)ethanone Show/Hide	C26H29N7O2	1
1	GI50 = 3800 nM Bioactivity Info	TI LI LO TS
CP0009734 Compound Info	4-amino-2-(4-morpholin-4-ylphenyl)thieno[3,2-c]pyridine-7-carboxamide Show/Hide	C18H18N4O2S	1
1	IC50 = 748 nM Bioactivity Info	TI LI LO TS
CP0008918 Compound Info	4-amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-methylthieno[3,2-c]pyridine-7-carboxamide Show/Hide	C19H22N4O3S2	1
1	IC50 = 1090 nM Bioactivity Info	TI LI LO TS
CP0392929 Compound Info	4-amino-2-[4-(2-cyanopropan-2-yl)phenyl]-N-methylthieno[3,2-c]pyridine-7-carboxamide Show/Hide	C19H18N4OS	1
1	IC50 = 1160 nM Bioactivity Info	TI LI LO TS
CP0441323 Compound Info	4-amino-N-methyl-2-(4-morpholin-4-ylphenyl)thieno[3,2-c]pyridine-7-carboxamide Show/Hide	C19H20N4O2S	1
1	IC50 = 1810 nM Bioactivity Info	TI LI LO TS
CP0001781 Compound Info	4-amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-methoxyethyl)thieno[3,2-c]pyridine-7-carboxamide Show/Hide	C21H26N4O4S2	1
1	IC50 = 6610 nM Bioactivity Info	TI LI LO TS
CP0441325 Compound Info	4-amino-N-methyl-2-[4-(trifluoromethoxy)phenyl]thieno[3,2-c]pyridine-7-carboxamide Show/Hide	C16H12F3N3O2S	1
1	IC50 = 6850 nM Bioactivity Info	TI LI LO TS
CP0417018 Compound Info	4-amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(3-morpholin-4-ylpropyl)thieno[3,2-c]pyridine-7-carboxamide Show/Hide	C25H33N5O4S2	1
1	IC50 = 12600 nM Bioactivity Info	TI LI LO TS
CP0001071 Compound Info	4-amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-[2-(dimethylamino)ethyl]thieno[3,2-c]pyridine-7-carboxamide Show/Hide	C22H29N5O3S2	1
1	IC50 > 25000 nM Bioactivity Info	TI LI LO TS
CP0392981 Compound Info	4-amino-N-methyl-2-(4-methylphenyl)thieno[3,2-c]pyridine-7-carboxamide Show/Hide	C16H15N3OS	1
1	IC50 > 25000 nM Bioactivity Info	TI LI LO TS
CP0417017 Compound Info	4-amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-piperidin-1-ylethyl)thieno[3,2-c]pyridine-7-carboxamide Show/Hide	C25H33N5O3S2	1
1	IC50 > 25000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000743 , CellSensor STAT6-bla RA-1

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000157 , NCI-H1975

Cell Line Info

Cell Line ID: CL000012 , Sf21

Cell Line Info

Cell Line ID: CL000013 , Sf9

Cell Line Info

Cell Line ID: CL000128 , TF-1

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0102068 Compound Info	CHEMBL3780091 Show/Hide	C18H21N5O	1
1	IC50 = 0.1 nM
CP0807417 Compound Info	4-(((2S,4S)-1-(4-Chlorobenzyl)-2-methylpiperidin-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide Show/Hide	C22H26ClN5O	1
1	IC50 = 0.145 nM
CP0012129 Compound Info	INCB-018424 Show/Hide	C17H18N6	17
1	IC50 = 0.43 nM
2	IC50 = 0.6 nM
3	IC50 = 0.8 nM
4	IC50 = 1.1 nM
5	IC50 = 1.2 nM
6	IC50 = 3 nM
7	IC50 = 3.2 nM
8	IC50 = 3.3 nM
9	IC50 = 6 nM
10	IC50 = 6.4 nM
11	IC50 = 7 nM
12	IC50 = 38 nM
13	IC50 = 1053 nM
14	Kd = 3.4 nM
15	Kd > 10000 nM
16	Ki = 0.09 nM
17	Ki = 0.2 nM
CP0002393 Compound Info	3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile Show/Hide	C16H20N6O	26
1	IC50 = 0.5 nM
2	IC50 = 0.8 nM
3	IC50 = 1.3 nM
4	IC50 = 1.4 nM
5	IC50 = 1.42 nM
6	IC50 = 1.55 nM
7	IC50 = 1.6 nM
8	IC50 = 1.7 nM
9	IC50 = 2 nM
10	IC50 = 3 nM
11	IC50 = 3.1 nM
12	IC50 = 3.2 nM
13	IC50 = 3.3 nM
14	IC50 = 3.7 nM
15	IC50 = 3.8 nM
16	IC50 = 4.1 nM
17	IC50 = 15 nM
18	IC50 = 15.1 nM
19	IC50 = 33 nM
20	IC50 = 74 nM
21	IC50 = 112 nM
22	Kd = 1.6 nM
23	Kd = 1.7 nM
24	Kd > 10000 nM
25	Ki = 0.68 nM
26	Ki = 0.7 nM
CP0807416 Compound Info	4-((cis-3-Fluoro-1-(3-methoxybenzyl)piperidin-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide Show/Hide	C22H26FN5O2	1
1	IC50 = 0.769 nM
CP0158332 Compound Info	CHEMBL3780467 Show/Hide	C20H27N5O3	1
1	IC50 = 0.8 nM
CP0004109 Compound Info	Bms-986165 Show/Hide	C20H22N8O3	2
1	IC50 = 1 nM
2	IC50 > 10000 nM
CP0692982 Compound Info	[(1R,2R,4R,5S)-5-(3-Methyl-6-oxo-1,2,7-triaza-2,7-dihydroinden-4-yl)-2-norbornanyl]acetonitrile Show/Hide	C16H18N4O	1
1	IC50 = 1 nM
CP0952685 Compound Info	4-((trans-1-(3-Chlorobenzyl)-2-methylpiperidin-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide Show/Hide	C22H26ClN5O	1
1	IC50 = 1.12 nM
CP0701646 Compound Info	rac-3-Methyl-4-[trans-4-[2-oxo-2-(3-phenylpyrrolidin-1-yl)-ethyl]cyclohexyl]-2,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C25H30N4O2	1
1	IC50 = 2.1 nM
CP0146867 Compound Info	CHEMBL2322135 Show/Hide	C14H16N4	1
1	IC50 = 3 nM
CP0712228 Compound Info	4-[trans-4-[2-(3-Benzylazetidin-1-yl)-2-oxo-ethyl]-cyclohexyl]-3-methyl-2,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C25H30N4O2	1
1	IC50 = 3 nM
CP0812653 Compound Info	4-[trans-4-[2-(4,4-Dimethyl-1-piperidyl)-2-oxo-ethyl]-cyclohexyl]-3-methyl-2,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C22H32N4O2	1
1	IC50 = 3.4 nM
CP0130638 Compound Info	12-cyclohexyl-1,5,7,10-tetrazatricyclo[7.3.0.02,6]dodeca-2(6),3,7,9,11-pentaene Show/Hide	C14H16N4	1
1	IC50 = 4 nM
CP0014161 Compound Info	2-[[5-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)furan-2-yl]methylidene]propanedinitrile Show/Hide	C22H18N6O	1
1	IC50 = 4 nM
CP0640933 Compound Info	ABROCITINIB Show/Hide	C14H21N5O2S	2
1	IC50 = 5.1 nM
2	IC50 = 29 nM
CP0692980 Compound Info	(1S)-2,2-Difluoro-N-[trans-4-(3-methyl-6-oxo-2,7-dihydropyrazolo[3,4-b]pyridin-4-yl)cyclohexyl]-cyclopropanecarboxamide Show/Hide	C17H20F2N4O2	1
1	IC50 = 6.4 nM
CP0952760 Compound Info	4-((1-(3-Chlorobenzyl)azepan-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide Show/Hide	C22H26ClN5O	1
1	IC50 = 9.43 nM
CP0146866 Compound Info	12-cyclohexyl-1,5,7,11-tetrazatricyclo[7.3.0.02,6]dodeca-2(6),3,7,9,11-pentaene Show/Hide	C14H16N4	1
1	IC50 = 10 nM
CP0008628 Compound Info	US10112907, Example 00033 Show/Hide	C21H23N5O3S	8
1	IC50 = 10 nM
2	IC50 = 26.2 nM
3	IC50 = 33 nM
4	IC50 = 115 nM
5	IC50 = 363 nM
6	IC50 = 629 nM
7	IC50 = 636 nM
8	Kd = 11 nM
CP0692981 Compound Info	[(1S,2S,4S,5R)-5-(3-Methyl-6-oxo-1,2,7-triaza-2,7-dihydroinden-4-yl)-2-norbornanyl]acetonitrile Show/Hide	C16H18N4O	1
1	IC50 = 11 nM
CP0812652 Compound Info	rac-1-[2-[trans-4-(3-Methyl-6-oxo-2,7-dihydropyrazolo[3,4-b]-pyridin-4-yl)cyclohexyl]acetyl]pyrrolidine-3-carbonitrile Show/Hide	C20H25N5O2	1
1	IC50 = 11 nM
CP0013024 Compound Info	(E)-3-[5-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)furan-2-yl]prop-2-enenitrile Show/Hide	C21H19N5O	1
1	IC50 = 12 nM
CP0701642 Compound Info	1-[2-[trans-4-(3-Methyl-6-oxo-2,7-dihydropyrazolo[3,4-b]-pyridin-4-yl)cyclohexyl]acetyl]azetidine-3-carbonitrile Show/Hide	C19H23N5O2	1
1	IC50 = 13 nM
CP0701645 Compound Info	[trans-4-(3-Methyl-6-oxo-2,7-dihydropyrazolo[3,4-b]-pyridin-4-yl)cyclohexyl] (1S)-2,2-difluorocyclopropanecarboxylate Show/Hide	C17H19F2N3O3	1
1	IC50 = 14 nM
CP0807413 Compound Info	4-((8-(4-Chlorobenzyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide Show/Hide	C23H26ClN5O	1
1	IC50 = 17.4 nM
CP0130641 Compound Info	CHEMBL2322137 Show/Hide	C14H15N3O	1
1	IC50 = 20 nM
CP0146865 Compound Info	3-cyclohexyl-4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C15H18N4	2
1	IC50 = 20 nM
2	Ki = 1.3 nM
CP0007710 Compound Info	2-[[1-[2-fluoro-4-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]phenyl]piperidin-4-yl]-methylamino]ethanol Show/Hide	C25H34FN7O	1
1	IC50 = 26 nM
CP0108248 Compound Info	12-cyclohexyl-1,5,7,10,11-pentazatricyclo[7.3.0.02,6]dodeca-2(6),3,7,9,11-pentaene Show/Hide	C13H15N5	1
1	IC50 = 30 nM
CP0168169 Compound Info	1-cyclohexyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine (2) Show/Hide	C14H16N4	1
1	IC50 = 30 nM
CP0768026 Compound Info	[(1S,2R,4S,5R)-5-(3-Methyl-6-oxo-1,2,7-triaza-2,7-dihydroinden-4-yl)-2-norbornanyl]acetonitrile Show/Hide	C16H18N4O	1
1	IC50 = 30 nM
CP0693222 Compound Info	3-[trans-4-(3-Methyl-6-oxo-2,7-dihydropyrazolo[3,4-b]-pyridin-4-yl)cyclohexyl]propanenitrile Show/Hide	C16H20N4O	1
1	IC50 = 32 nM
CP0146014 Compound Info	3-cyclohexyl-4-(trifluoromethyl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C15H15F3N4	1
1	IC50 = 40 nM
CP0692983 Compound Info	rac-3-Methyl-4-[(1S,2R)-2-methylcyclohexyl]-2,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C14H19N3O	1
1	IC50 = 40 nM
CP0692984 Compound Info	2-[trans-4-(3-Methyl-6-oxo-2,7-dihydropyrazolo[3,4-b]-pyridin-4-yl)cyclohexyl]acetonitrile Show/Hide	C15H18N4O	1
1	IC50 = 40 nM
CP0812651 Compound Info	1-Cyclobutyl-N-[trans-4-(3-methyl-6-oxo-2,7-dihydropyrazolo[3,4-b]pyridin-4-yl)cyclohexyl]-methanesulfonamide Show/Hide	C18H26N4O3S	1
1	IC50 = 40 nM
CP0233890 Compound Info	ABT-494 Show/Hide	C17H19F3N6O	1
1	IC50 = 43 nM
CP0701647 Compound Info	rac-3-Methyl-4-[(1R,2R,4S*)-norbornan-2-yl]-2,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C14H17N3O	1
1	IC50 = 44 nM
CP0701648 Compound Info	rac-3-Methyl-4-[(1R,2S,4S*)-norbornan-2-yl]-2,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C14H17N3O	1
1	IC50 = 46 nM
CP0701643 Compound Info	[(1R,2S,4R,5S)-5-(3-Methyl-6-oxo-1,2,7-triaza-2,7-dihydroinden-4-yl)-2-norbornanyl]acetonitrile Show/Hide	C16H18N4O	1
1	IC50 = 47 nM
CP0633840 Compound Info	(E/Z)-2-Cyano-3-(5-(1-cyclohexyl-1,6-dihydroimidazo[4,5-d]-pyrrolo[2,3-b]pyridin-2-yl)furan-2-yl)-N,N-dimethylacrylamide Show/Hide	C24H24N6O2	2
1	IC50 = 52 nM
2	IC50 = 668 nM
CP0701641 Compound Info	rac-4-(2-Bicyclo[2.2.2]octanyl)-3-methyl-2,7-dihydropyrazolo-[3,4-b]pyridin-6-one Show/Hide	C15H19N3O	1
1	IC50 = 54 nM
CP0351745 Compound Info	Cyclopropanecarboxylic acid {5-[4-(3-cyano-azetidine-1- carbonyl)-phenyl]- [1,2,4]triazolo[1,5-a]pyridin-2- yl)-amide Show/Hide	C21H18N6O2	1
1	IC50 = 61 nM
CP0207730 Compound Info	4-cyclopentyl-3-methyl-2,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C12H15N3O	1
1	IC50 = 72 nM
CP0689277 Compound Info	(2R)-N-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propanamide Show/Hide	C25H31N9O2	1
1	IC50 = 73 nM
CP0768025 Compound Info	(1R)-2,2-Difluoro-N-[trans-4-(3-methyl-6-oxo-2,7-dihydropyrazolo[3,4-b]pyridin-4-yl)cyclohexyl]-cyclopropanecarboxamide Show/Hide	C17H20F2N4O2	1
1	IC50 = 78 nM
CP0146868 Compound Info	CHEMBL2322136 Show/Hide	C15H18N4	1
1	IC50 = 90 nM
CP0232448 Compound Info	N-[5-[4-(2-cyano-1-hydroxyprop-2-enyl)phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide Show/Hide	C20H17N5O2	1
1	IC50 = 95 nM
CP0701644 Compound Info	N-[trans-4-(3-Methyl-6-oxo-2,7-dihydropyrazolo[3,4-b]-pyridin-4-yl)cyclohexyl]cyclopentanecarboxamide Show/Hide	C19H26N4O2	1
1	IC50 = 110 nM
CP0637281 Compound Info	(E/Z)-3-(5-(1-Cyclohexyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]-pyridin-2-yl)furan-2-yl)-2-(4-methylpiperazine-1-carbonyl)-acrylonitrile Show/Hide	C27H29N7O2	1
1	IC50 = 117 nM
CP0124474 Compound Info	4-(cyclobutylmethyl)-3-methyl-2,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C12H15N3O	1
1	IC50 = 120 nM
CP0330677 Compound Info	4-cyclohexyl-3-methyl-2,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C13H17N3O	1
1	IC50 = 130 nM
CP0162855 Compound Info	4-cyclohexyl-5-(hydroxymethyl)-3-methyl-2,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C14H19N3O2	1
1	IC50 = 140 nM
CP0735624 Compound Info	N-[trans-4-(3-Methyl-6-oxo-2,7-dihydropyrazolo[3,4-b]-pyridin-4-yl)cyclohexyl]cyclopropanecarboxamide Show/Hide	C17H22N4O2	1
1	IC50 = 220 nM
CP0207734 Compound Info	4-cyclohexyl-3-ethyl-2,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C14H19N3O	1
1	IC50 = 460 nM
CP0356130 Compound Info	4-cyclohexyl-5-(2-hydroxyethyl)-3-methyl-2,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C15H21N3O2	1
1	IC50 = 490 nM
CP0812656 Compound Info	4-(4-trans-Hydroxycyclohexyl)-3-methyl-2,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C13H17N3O2	1
1	IC50 = 490 nM
CP0162853 Compound Info	4-cyclohexyl-3-cyclopropyl-2,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C15H19N3O	1
1	IC50 = 500 nM
CP0692985 Compound Info	4-(4-trans-Aminocyclohexyl)-3-methyl-2,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C13H18N4O	1
1	IC50 = 820 nM
CP0712223 Compound Info	N-Cyclopropyl-trans-4-(3-methyl-6-oxo-2,7-dihydropyrazolo[3,4-b]pyridin-4-yl)cyclohexanecarboxamide Show/Hide	C17H22N4O2	1
1	IC50 = 2000 nM
CP0330676 Compound Info	4-cyclohexyl-3-methyl-6-oxo-2,7-dihydropyrazolo[3,4-b]pyridine-5-carbonitrile Show/Hide	C14H16N4O	1
1	IC50 = 2100 nM
CP0330675 Compound Info	3-methyl-4-phenyl-2,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C13H11N3O	1
1	IC50 = 2200 nM
CP0207733 Compound Info	4-cyclohexyl-1,7-dihydropyrazolo[3,4-b]pyridin-6-one Show/Hide	C12H15N3O	1
1	IC50 = 15000 nM
CP0007430 Compound Info	IBRUTINIB Show/Hide	C25H24N6O2	1
1	IC50 > 10000 nM
CP0031719 Compound Info	(R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine Show/Hide	C21H22Cl2FN5O	2
1	Kd = 330 nM
2	Kd > 10000 nM
CP0108652 Compound Info	CHEMBL2386635 Show/Hide	C18H21N5O	1
1	Ki = 0.1 nM
CP0088219 Compound Info	N-[[3-[(1R,2R,4S)-2-bicyclo[2.2.1]heptanyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]methanesulfonamide Show/Hide	C17H21N5O2S	1
1	Ki = 0.2 nM
CP0087139 Compound Info	CHEMBL2386636 Show/Hide	C19H23N5O	1
1	Ki = 0.3 nM
CP0186393 Compound Info	3-oxo-3-[(3R)-3-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrile Show/Hide	C16H16N6O	1
1	Ki = 0.4 nM
CP0079525 Compound Info	3-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrile Show/Hide	C16H18N6	1
1	Ki = 0.6 nM
CP0329529 Compound Info	N-[2-[3-(2-bicyclo[2.2.1]heptanyl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethyl]methanesulfonamide Show/Hide	C18H23N5O2S	1
1	Ki = 0.6 nM
CP0084964 Compound Info	CHEMBL2386629 Show/Hide	C18H22F3N5O	1
1	Ki = 0.8 nM
CP0266379 Compound Info	(1R)-1-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)ethanol Show/Hide	C16H20N4O	1
1	Ki = 0.8 nM
CP0255798 Compound Info	3-[4-(4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrile Show/Hide	C17H20N6	1
1	Ki = 0.9 nM
CP0261449 Compound Info	CHEMBL2386634 Show/Hide	C17H19N5O	1
1	Ki = 0.9 nM
CP0084967 Compound Info	(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)methanol Show/Hide	C15H18N4O	1
1	Ki = 1.1 nM
CP0265330 Compound Info	CHEMBL2386630 Show/Hide	C18H23F2N5O	1
1	Ki = 1.1 nM
CP0355897 Compound Info	3-(1-methylsulfonylpiperidin-4-yl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C14H17N5O2S	1
1	Ki = 1.2 nM
CP0315771 Compound Info	3-[(3R,4R)-3-fluoropiperidin-4-yl]-4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C14H16FN5	1
1	Ki = 1.2 nM
CP0285868 Compound Info	(1R)-1-[3-[(1S,3S)-3-(2,2,2-trifluoroethylamino)cyclopentyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethanol Show/Hide	C17H20F3N5O	1
1	Ki = 1.2 nM
CP0260731 Compound Info	3-(1-benzylpiperidin-4-yl)-4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C21H23N5	1
1	Ki = 1.3 nM
CP0178056 Compound Info	CHEMBL2159205 Show/Hide	C18H22N6	1
1	Ki = 1.5 nM
CP0108702 Compound Info	CHEMBL2392500 Show/Hide	C15H15N7O	1
1	Ki = 1.5 nM
CP0369955 Compound Info	(1S)-1-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)ethane-1,2-diol Show/Hide	C16H20N4O2	1
1	Ki = 1.6 nM
CP0255709 Compound Info	3-(4-methyl-1-methylsulfonylpiperidin-4-yl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C15H19N5O2S	1
1	Ki = 1.7 nM
CP0270257 Compound Info	N-[2-[3-[1-(2-cyanoethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethyl]methanesulfonamide Show/Hide	C19H25N7O2S	1
1	Ki = 1.7 nM
CP0120553 Compound Info	(1R,3R)-3-(4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexan-1-ol Show/Hide	C15H18N4O	1
1	Ki = 1.8 nM
CP0359333 Compound Info	(1R)-1-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)propan-1-ol Show/Hide	C17H22N4O	1
1	Ki = 1.8 nM
CP0102822 Compound Info	CHEMBL2386633 Show/Hide	C17H19N5O	1
1	Ki = 1.9 nM
CP0339507 Compound Info	3-[1-(pyrimidin-5-ylmethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C18H19N7	1
1	Ki = 2 nM
CP0315770 Compound Info	3-(3,3-difluoropiperidin-4-yl)-4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C14H15F2N5	1
1	Ki = 2 nM
CP0087579 Compound Info	(1R)-1-[3-[(1S,3R)-3-(2,2,2-trifluoroethylamino)cyclopentyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethanol Show/Hide	C17H20F3N5O	1
1	Ki = 2 nM
CP0261451 Compound Info	(1R)-1-[3-(1-ethyl-3,3-difluoropiperidin-4-yl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethanol Show/Hide	C17H21F2N5O	1
1	Ki = 2 nM
CP0171798 Compound Info	N-[2-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)ethyl]methanesulfonamide Show/Hide	C17H23N5O2S	1
1	Ki = 2.1 nM
CP0086382 Compound Info	CHEMBL2392488 Show/Hide	C15H17N7	1
1	Ki = 2.1 nM
CP0247748 Compound Info	3-(1-benzylpiperidin-4-yl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C20H21N5	1
1	Ki = 2.4 nM
CP0104959 Compound Info	CHEMBL2392485 Show/Hide	C17H22N6O2	1
1	Ki = 2.4 nM
CP0159699 Compound Info	CHEMBL2159208 Show/Hide	C17H21N5O2	1
1	Ki = 2.6 nM
CP0088169 Compound Info	N-[(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)methyl]methanesulfonamide Show/Hide	C16H21N5O2S	1
1	Ki = 2.6 nM
CP0323372 Compound Info	N-[2-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)ethyl]acetamide Show/Hide	C18H23N5O	1
1	Ki = 2.6 nM
CP0266378 Compound Info	(1R)-1-[3-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethanol Show/Hide	C17H20F3N5O	1
1	Ki = 2.6 nM
CP0356271 Compound Info	CHEMBL2152422 Show/Hide	C15H19N5O2S	1
1	Ki = 2.7 nM
CP0198952 Compound Info	(1R,3R)-3-[4-[(1R)-1-hydroxyethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]cyclohexan-1-ol Show/Hide	C16H20N4O2	1
1	Ki = 2.7 nM
CP0142992 Compound Info	4-methyl-3-[(3S)-oxan-3-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C14H16N4O	1
1	Ki = 2.8 nM
CP0108487 Compound Info	(1R)-1-[3-[(3S)-oxan-3-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethanol Show/Hide	C15H18N4O2	1
1	Ki = 2.8 nM
CP0335391 Compound Info	3-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C15H16F3N5	1
1	Ki = 2.9 nM
CP0175649 Compound Info	3-[4-(4-cyclopropyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrile Show/Hide	C19H22N6	1
1	Ki = 2.9 nM
CP0204289 Compound Info	N-[[3-(2-bicyclo[2.2.1]heptanyl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]acetamide Show/Hide	C18H21N5O	1
1	Ki = 3 nM
CP0179649 Compound Info	methyl N-[(1R,3R)-3-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclopentyl]carbamate Show/Hide	C15H17N5O2	1
1	Ki = 3.2 nM
CP0329462 Compound Info	N-[(3-cycloheptyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)methyl]methanesulfonamide Show/Hide	C17H23N5O2S	1
1	Ki = 3.3 nM
CP0369957 Compound Info	3-[4-[4-[(1R)-1-hydroxyethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]propanenitrile Show/Hide	C18H22N6O	1
1	Ki = 3.4 nM
CP0266430 Compound Info	2-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)ethanol Show/Hide	C16H20N4O	1
1	Ki = 3.5 nM
CP0302958 Compound Info	tert-butyl N-[(1S,3R)-3-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclopentyl]carbamate Show/Hide	C18H23N5O2	1
1	Ki = 3.7 nM
CP0369175 Compound Info	N-[2-[3-[1-(2-cyanoethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethyl]acetamide Show/Hide	C20H25N7O	1
1	Ki = 3.7 nM
CP0120790 Compound Info	N-[[3-[(1S,2S,4R)-2-bicyclo[2.2.1]heptanyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]methanesulfonamide Show/Hide	C17H21N5O2S	1
1	Ki = 3.8 nM
CP0274272 Compound Info	N-[[3-[(1R,3R)-3-hydroxycyclohexyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]methanesulfonamide Show/Hide	C16H21N5O3S	1
1	Ki = 4.2 nM
CP0426744 Compound Info	3-[4-(4-cyclobutyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrile Show/Hide	C20H24N6	1
1	Ki = 4.3 nM
CP0359605 Compound Info	CHEMBL2152420 Show/Hide	C17H20N6	1
1	Ki = 4.5 nM
CP0178055 Compound Info	CHEMBL2159206 Show/Hide	C16H21N5O2S	1
1	Ki = 4.5 nM
CP0334795 Compound Info	3-[4-(4-propyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrile Show/Hide	C19H24N6	1
1	Ki = 4.6 nM
CP0086380 Compound Info	CHEMBL2392484 Show/Hide	C18H24N6O	1
1	Ki = 4.7 nM
CP0120685 Compound Info	(1R,3R)-3-(4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclopentan-1-ol Show/Hide	C14H16N4O	1
1	Ki = 4.8 nM
CP0107727 Compound Info	CHEMBL2386628 Show/Hide	C17H22N4O2	1
1	Ki = 4.9 nM
CP0088171 Compound Info	N-[[3-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]methanesulfonamide Show/Hide	C17H21F3N6O2S	1
1	Ki = 5 nM
CP0265331 Compound Info	3-[(3R)-3-[4-[(1R)-1-hydroxyethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]-3-oxopropanenitrile Show/Hide	C18H20N6O2	1
1	Ki = 5.2 nM
CP0323371 Compound Info	N-[(3-cyclopentyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)methyl]methanesulfonamide Show/Hide	C15H19N5O2S	1
1	Ki = 5.3 nM
CP0120684 Compound Info	(1R,3S)-3-(4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclopentan-1-ol Show/Hide	C14H16N4O	1
1	Ki = 5.4 nM
CP0323227 Compound Info	N-[[3-[1-(2-cyanoethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]-2-methylpropane-1-sulfonamide Show/Hide	C21H29N7O2S	1
1	Ki = 5.4 nM
CP0261450 Compound Info	CHEMBL2386625 Show/Hide	C16H20N4O2	1
1	Ki = 5.4 nM
CP0340065 Compound Info	CHEMBL2152414 Show/Hide	C14H17N5	1
1	Ki = 5.8 nM
CP0178017 Compound Info	CHEMBL2159209 Show/Hide	C15H18N4O	1
1	Ki = 5.8 nM
CP0270172 Compound Info	CHEMBL2152421 Show/Hide	C22H22N6	1
1	Ki = 5.9 nM
CP0086377 Compound Info	CHEMBL2392480 Show/Hide	C16H19N7	1
1	Ki = 5.9 nM
CP0079526 Compound Info	CHEMBL2152413 Show/Hide	C19H25N5O2	1
1	Ki = 6.1 nM
CP0335392 Compound Info	CHEMBL2152412 Show/Hide	C19H25N5O2	1
1	Ki = 6.1 nM
CP0315772 Compound Info	CHEMBL2159207 Show/Hide	C17H21N5O	1
1	Ki = 6.1 nM
CP0086379 Compound Info	CHEMBL2392489 Show/Hide	C13H16N6O2S	1
1	Ki = 6.2 nM
CP0161562 Compound Info	CHEMBL2159212 Show/Hide	C15H18N4O	1
1	Ki = 6.7 nM
CP0285853 Compound Info	(1R)-1-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)ethane-1,2-diol Show/Hide	C16H20N4O2	1
1	Ki = 7.2 nM
CP0315684 Compound Info	(1R,3S)-3-(4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexan-1-ol Show/Hide	C15H18N4O	1
1	Ki = 7.3 nM
CP0345485 Compound Info	N-[[3-[1-(2-cyanoethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]methanesulfonamide Show/Hide	C18H23N7O2S	1
1	Ki = 7.3 nM
CP0305359 Compound Info	CHEMBL2392493 Show/Hide	C14H18N6O2S	1
1	Ki = 7.9 nM
CP0186394 Compound Info	3-[4-methyl-1-(pyrimidin-5-ylmethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C19H21N7	1
1	Ki = 8.3 nM
CP0369176 Compound Info	ethyl N-[[3-[1-(2-cyanoethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]carbamate Show/Hide	C20H25N7O2	1
1	Ki = 8.4 nM
CP0217586 Compound Info	CHEMBL2392487 Show/Hide	C19H20N6	1
1	Ki = 8.5 nM
CP0247830 Compound Info	3-[4-[4-[2-(oxolan-2-yl)ethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]propanenitrile Show/Hide	C22H28N6O	1
1	Ki = 8.7 nM
CP0310453 Compound Info	3-[4-(4-propan-2-yl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrile Show/Hide	C19H24N6	1
1	Ki = 9.1 nM
CP0257219 Compound Info	CHEMBL2152419 Show/Hide	C18H23N5	1
1	Ki = 9.3 nM
CP0178020 Compound Info	3-[(3S,4R)-3-fluoropiperidin-4-yl]-4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C14H16FN5	1
1	Ki = 9.3 nM
CP0247820 Compound Info	3-[4-[4-[2-(1-methylimidazol-2-yl)ethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]propanenitrile Show/Hide	C22H26N8	1
1	Ki = 9.3 nM
CP0508197 Compound Info	CHEMBL2151053 Show/Hide	C16H19N5O2	1
1	Ki = 9.5 nM
CP0165766 Compound Info	3-[1-(benzenesulfonyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C19H19N5O2S	1
1	Ki = 9.6 nM
CP0334376 Compound Info	CHEMBL2152415 Show/Hide	C14H17N5	1
1	Ki = 9.8 nM
CP0100650 Compound Info	4-methyl-3-piperidin-4-yl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C14H17N5	1
1	Ki = 10 nM
CP0329463 Compound Info	N-[(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)methyl]acetamide Show/Hide	C17H21N5O	1
1	Ki = 10 nM
CP0107726 Compound Info	(1S)-1-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)ethanol Show/Hide	C16H20N4O	1
1	Ki = 10 nM
CP0186640 Compound Info	[(2S)-1-methylpiperidin-2-yl]-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]methanone Show/Hide	C20H26N6O	1
1	Ki = 11 nM
CP0334377 Compound Info	CHEMBL2152418 Show/Hide	C18H23N5O	1
1	Ki = 11 nM
CP0356714 Compound Info	CHEMBL2152416 Show/Hide	C18H23N5O	1
1	Ki = 12 nM
CP0345484 Compound Info	N-[[3-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]acetamide Show/Hide	C18H21F3N6O	1
1	Ki = 12 nM
CP0369956 Compound Info	CHEMBL2386626 Show/Hide	C16H20N4O2	1
1	Ki = 12 nM
CP0087922 Compound Info	CHEMBL2392486 Show/Hide	C14H16N6O2	1
1	Ki = 12 nM
CP0104957 Compound Info	CHEMBL2392483 Show/Hide	C15H18N6O2	1
1	Ki = 12 nM
CP0339771 Compound Info	CHEMBL2392499 Show/Hide	C13H15N5O	1
1	Ki = 12 nM
CP0194789 Compound Info	CHEMBL2152423 Show/Hide	C17H21N5O2	1
1	Ki = 13 nM
CP0106619 Compound Info	3-[4-[4-[2-(1-methylpyrazol-3-yl)ethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]propanenitrile Show/Hide	C22H26N8	1
1	Ki = 13 nM
CP0100646 Compound Info	2-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)propan-2-ol Show/Hide	C17H22N4O	1
1	Ki = 13 nM
CP0274441 Compound Info	3-[4-[4-(2-pyrazol-1-ylethyl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]propanenitrile Show/Hide	C21H24N8	1
1	Ki = 14 nM
CP0257242 Compound Info	[(2S)-1-methylpyrrolidin-2-yl]-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]methanone Show/Hide	C19H24N6O	1
1	Ki = 15 nM
CP0076053 Compound Info	3-[4-[4-(cyclopentylmethyl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]propanenitrile Show/Hide	C22H28N6	1
1	Ki = 16 nM
CP0207474 Compound Info	N-[[3-[1-(2-cyanoethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]acetamide Show/Hide	C19H23N7O	1
1	Ki = 16 nM
CP0112715 Compound Info	(1S)-1-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)propan-1-ol Show/Hide	C17H22N4O	1
1	Ki = 16 nM
CP0157841 Compound Info	CHEMBL2392490 Show/Hide	C18H19N7	1
1	Ki = 16 nM
CP0274109 Compound Info	phenyl-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]methanone Show/Hide	C20H19N5O	1
1	Ki = 18 nM
CP0159700 Compound Info	4-methyl-3-(oxan-4-yl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C14H16N4O	1
1	Ki = 18 nM
CP0079522 Compound Info	3-oxo-3-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrile Show/Hide	C16H16N6O	1
1	Ki = 19 nM
CP0217584 Compound Info	CHEMBL2392498 Show/Hide	C13H16N6	1
1	Ki = 21 nM
CP0355898 Compound Info	[(2S)-1-propan-2-ylpyrrolidin-2-yl]-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]methanone Show/Hide	C21H28N6O	1
1	Ki = 22 nM
CP0369177 Compound Info	3-[4-[4-(oxolan-2-ylmethyl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]propanenitrile Show/Hide	C21H26N6O	1
1	Ki = 24 nM
CP0282470 Compound Info	3-methyl-1-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]butan-1-one Show/Hide	C18H23N5O	1
1	Ki = 28 nM
CP0284087 Compound Info	N-[[3-(7-oxabicyclo[2.2.1]heptan-2-yl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]methanesulfonamide Show/Hide	C16H19N5O3S	1
1	Ki = 28 nM
CP0351812 Compound Info	2-(dimethylamino)-1-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]ethanone Show/Hide	C17H22N6O	1
1	Ki = 32 nM
CP0088180 Compound Info	3-[4-[4-(oxan-4-ylmethyl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]propanenitrile Show/Hide	C22H28N6O	1
1	Ki = 43 nM
CP0112719 Compound Info	3-piperidin-4-yl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C13H15N5	2
1	Ki = 45 nM
2	Ki = 46 nM
CP0321389 Compound Info	3-(1-ethylpiperidin-4-yl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C15H19N5	1
1	Ki = 50 nM
CP0066334 Compound Info	2,6-dichloro-N-[2-(cyclopropanecarbonylamino)pyridin-4-yl]benzamide Show/Hide	C16H13Cl2N3O2	2
1	Ki = 83.8 nM
2	Ki = 84 nM
CP0525615 Compound Info	3-(4-methylpiperidin-4-yl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene Show/Hide	C14H17N5	1
1	Ki = 96 nM
CP0194788 Compound Info	CHEMBL2152417 Show/Hide	C18H23N5O	1
1	Ki = 280 nM

Clinical Information about the Protein

Target 1 ( Janus kinase 1 (JAK-1) )

Target Type	Successful Target
Disease	9 Target-related Diseases				9
1	Rheumatoid arthritis [ICD-11: FA20]
2	High-risk myelofibrosis [ICD-11: 2A20.2]
3	Myelofibrosis [ICD-11: 2A20.2]
4	Atopic dermatitis [ICD-11: EA80]
5	Malignant neoplasm [ICD-11: 2A00-2F9Z]
6	Asthma [ICD-11: CA23]
7	B-cell lymphoma [ICD-11: 2A86]
8	Systemic lupus erythematosus [ICD-11: 4A40.0]
9	Diffuse large B-cell lymphoma [ICD-11: 2A81]
Approved Drug(s)	5 Approved Drugs				5
1	Baricitinib	Drug Info	Approved	Rheumatoid arthritis
2	Ruxolitinib	Drug Info	Approved	High-risk myelofibrosis
3	Momelotinib	Drug Info	Approved	Myelofibrosis
4	Abrocitinib	Drug Info	Approved	Atopic dermatitis
5	Upadacitinib	Drug Info	Approved	Rheumatoid arthritis
Clinical Trial Drug(s)	7 Clinical Trial Drugs				7
1	ATI-502	Drug Info	Phase 2	Atopic dermatitis
2	GLPG-0634	Drug Info	Phase 2	Rheumatoid arthritis
3	INCB039110	Drug Info	Phase 2	Malignant neoplasm
4	PF-06700841	Drug Info	Phase 2	Asthma
5	Cerdulatinib	Drug Info	Phase 2	B-cell lymphoma
6	GDC-0214	Drug Info	Phase 1	Asthma
7	GSK2586184	Drug Info	Phase 2	Systemic lupus erythematosus
Investigative Drug(s)	1 Investigative Drug				1
1	WHI-P154	Drug Info	Investigative	Diffuse large B-cell lymphoma

Target 2 ( HUMAN janus kinase 1 (JAK-1) )

Target Type	Unknown Type Target
Disease	1 Target-related Disease				1
1	Myelofibrosis [ICD-11: 2A22]
Clinical Trial Drug(s)	1 Clinical Trial Drug				1
1	Ruxolitinib	Drug Info	Approved	Myelofibrosis

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han