Search by Compound Name

Compound Name:

Compounds Sorted by Binding Data per Compound

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29
30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55
56 57 58 59 60 61 62 63 64 65 66 67 68 69 70 71 72 73 74 75 76 77 78 79 80 81
82 83 84 85 86 87 88 89 90 91 92 93 94 95 96 97 98 99 100 101 102 103 104 105
106 107 108 109 110 111 112 113 114 115 116 117 118 119 120 121 122 123 124
125 127 128 129 130 132 133 134 135 136 137 138 139 140 141 143 144 145 146
147 148 149 150 151 153 154 155 156 159 160 161 163 164 165 168 170 171 173
174 176 178 179 183 184 186 188 189 190 191 192 193 196 198 199 200 203 204
205 206 207 208 209 210 216 220 224 226 227 229 232 237 238 241 243 248 252
253 259 261 270 274 276 277 285 291 303 304 313 318 323 325 328 333 335 337
339 341 353 360 361 365 389 393 398 401 413 433 442 444 445 446 447 448 451
453 454 455 457 458 460 463 465 467 473 477 478 482 484 499 504 505 506 517
521 525 543 549 551 554 591 606 663 691 708 796 804 821 825 833 842 847 854
855 861 873 879 883 887 913 914 925 926 938 947 1010 1027 1050 1052 1081 1082
1099 1115 1130 1133 1206 1262 1543 1639 1903 2029
Compounds Sorted Alphabetically
Compound Name (alphabetical)
Enz. Inhib. Data
ITC Data
Binding Targets
Alternate Compound Names
2 IC50 18 Kd
  • Tyrosine-protein kinase JAK1
  • Tyrosine-protein kinase JAK2
  • Tyrosine-protein kinase JAK3
  • Tyrosine-protein kinase SYK
  • US10533001, Example Table 9a.1
  • US8501944, 370
  • US8501944, 374
  • US9868729, Example 38
2 IC50 18 Kd
  • Tyrosine-protein kinase JAK1
  • Tyrosine-protein kinase JAK2
  • Tyrosine-protein kinase JAK3
  • Tyrosine-protein kinase SYK
  • US10533001, Example Table 9a.4
  • US8501944, 373
  • US8501944, 376
  • US9868729, Example 254
20 Ki
  • Coagulation factor X
  • Coagulation factor XI
  • Coagulation factor XII
  • Complement C1r
  • Complement C1r subcomponent
  • Complement C1s
  • Factor XIIa
  • Plasma kallikrein
  • Plasminogen
  • Prothrombin
  • Tissue-type plasminogen activator
  • Transcription initiation factor IIA
  • Vitamin K-dependent protein C
  • US8598206, Table 6, 7
20 Ki
  • Coagulation factor X
  • Coagulation factor XI
  • Coagulation factor XII
  • Complement C1r
  • Complement C1s
  • Factor XIIa
  • Plasma kallikrein
  • Plasminogen
  • Prothrombin
  • Tissue-type plasminogen activator
  • Transcription initiation factor IIA
  • Vitamin K-dependent protein C
  • US8598206, Table 6, 19
7 Ki 13 IC50
  • 3-phosphoinositide dependent protein kinase-1
  • 5-hydroxytryptamine receptor 1A
  • 5-hydroxytryptamine receptor 1D
  • 5-hydroxytryptamine receptor 2B
  • 5-hydroxytryptamine receptor 2C
  • 5-hydroxytryptamine receptor 5A
  • 5-hydroxytryptamine receptor 7
  • Axin-1/Glycogen synthase kinase-3 beta
  • CDK2/Cyclin A/Cyclin A1
  • Cyclin-Dependent Kinase 1 (CDK1)
  • Cyclin-Dependent Kinase 5 (CDK5)
  • Cyclin-Dependent Kinase 9 (CDK9)
  • Cyclin-dependent kinase 1
  • Cyclin-dependent-like kinase 5
  • D(1B) dopamine receptor
  • Glycogen Synthase Kinase-3, beta
  • Muscarinic acetylcholine receptor M5
  • Sodium-dependent dopamine transporter
  • cAMP-Dependent Protein Kinase (PKA)
  • cGMP-Dependent Protein Kinase
  • 3-(2-aminopyrimidin-4-yl)-1H-indol-4-ol
  • Meridianin A
20 IC50
  • Activin receptor type-1
  • Activin receptor type-1B
  • Activin receptor type-1B/Activin receptor-like kinase 4 (ALK-4)
  • Activin receptor-like kinase 3 (ALK-3)
  • Bone morphogenetic protein receptor type-1B (BMPR1B) aa 168-495
  • Serine/threonine-protein kinase receptor R3
  • Serine/threonine-protein kinase receptor R3 (ALK1)
  • TGF-beta receptor type-1
  • US10017516, Compound 2
  • US9682983, 2
14 Ki 6 IC50
  • 72 kDa type IV collagenase
  • Carbonic Anhydrase IV
  • Carbonic anhydrase 1
  • Carbonic anhydrase 2
  • Collagenase (ChC)
  • Disintegrin and metalloproteinase domain-containing protein 17
  • Interstitial collagenase
  • Matrix metalloproteinase-12 (MMP12)
  • Matrix metalloproteinase-14 (MMP14)
  • Matrix metalloproteinase-7 (MMP7)
  • Matrix metalloproteinase-9
  • Meprin A subunit beta
  • Neutrophil collagenase
  • Stromelysin-1
  • CHEMBL83508
  • Hydroxamate 9
  • N-hydroxy-2-[(4-methoxybenzene)sulfonamido]acetamide
20 IC50
  • Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C
  • Homo sapiens phosphodiesterase 2A (PDE2A)
  • Phosphodiesterase 11A (PDE11A)
  • Phosphodiesterase 7B (PDE7B)
  • Phosphodiesterase 8
  • Phosphodiesterase 9A
  • cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
  • cAMP-specific 3',5'-cyclic phosphodiesterase 4B
  • cAMP-specific 3',5'-cyclic phosphodiesterase 7B
  • cGMP-inhibited 3',5'-cyclic phosphodiesterase B
  • cGMP-specific 3',5'-cyclic phosphodiesterase
  • US8741907, 3
  • US9067945, 2
16 Ki 2 IC50 2 EC50
  • 5-hydroxytryptamine receptor 1A
  • 5-hydroxytryptamine receptor 2A
  • 5-hydroxytryptamine receptor 2C
  • D(2) dopamine receptor
  • D(3) dopamine receptor
  • D(4) dopamine receptor
  • US8748608, 34
  • US8748608, 34 Enantiomer A
  • US8748608, 34 Enantiomer B
20 IC50
  • Leukocyte common antigen
  • Protein-Tyrosine Phosphatase 1B (PTP1B)
  • Protein-tyrosine phosphatase 1B
  • Tyrosine-protein phosphatase non-receptor type 2
  • 6-{4-[2-(1H-1,2,3-benzotriazol-1-yl)-3-{4-[difluoro(phosphono)methyl]phenyl}-2-phenylpropyl]phenyl}-2-(1-methoxy-3-methylbutyl)quinoline-8-phosphonic acid
  • Aryldifluoromethyl-Phosphonic Acid Inhibitor 11
  • CHEMBL266753
20 IC50
  • Aurora kinase A/B
  • Aurora kinase A/Targeting protein for Xklp2
  • Aurora kinase B
  • Aurora kinase B-A
  • Cyclin-dependent kinase 1
  • Epidermal growth factor receptor
  • Serine/threonine-protein kinase Aurora-A
  • Serine/threonine-protein kinase PLK1
  • 4-(4-(N-benzoylamino)anilino)-6-methoxy-7-(3-(1-morpholino)propoxy)-quinazoline
  • CHEMBL202721
  • N-[4-({6-methoxy-7-[3-(morpholin-4-yl)propoxy]quinazolin-4-yl}amino)phenyl]benzamide
  • ZM447439
20 IC50
  • Caspase-1
  • Caspase-10
  • Caspase-2
  • Caspase-3
  • Caspase-4
  • Caspase-5
  • Caspase-6
  • Caspase-7
  • Caspase-8
  • Caspase-9
  • US10167313, Compound 53
  • US9045524, 53
20 Ki
  • Orexin receptor type 1
  • Orexin receptor type 2
  • US9062078, 11
  • US9062078, 12A
  • US9062078, 12B
  • US9475819, 11
  • US9637496, 12B
  • US9695183, 12B
1 Ki 18 IC50 1 EC50
  • EZH1/PRC2
  • EZH2(Y641F)
  • EZH2/SUZ12/EED/RBBP7/RBBP4
  • Histone-lysine N-methyltransferase EZH2
  • US10155002, Compound 44
  • US10647700, Compound EPZ6438
  • US9090562, 143
  • US9090562, 44
  • US9394283, 1
8 Ki 12 IC50
  • P2X purinoceptor 7
  • P2X purinoceptor 7 (P2X7)
  • US10323032, Example 33
  • US9096596, 33
  • US9604982, Example 33
10 Ki 10 IC50
  • P2X purinoceptor 7
  • P2X purinoceptor 7 (P2X7)
  • US10053462, 33
  • US9102686, 33
  • US9540388, 32
1 Ki 18 IC50 1 EC50
  • HIV-1 Reverse Transcriptase
  • HIV-1 Reverse Transcriptase Mutant (L100I)
  • HIV-1 Reverse Transcriptase Mutant (Y181C)
  • Human immunodeficiency virus type 1 reverse transcriptase
  • Reverse transcriptase
  • 3-(5-bromopyridin-2-yl)-1-[2-(pyridin-2-yl)ethyl]thiourea hydrochloride
  • LY-300046 HCl
  • LY300046HCl
  • N-(2-(2-Pyridylethyl))-N -(2-(5-bromopyridyl))thiourea
  • PETT deriv.
  • Trovirdine
18 IC50 2 Kd
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5A (KDM5A(aa 1-1090)-Flag)
  • Lysine-specific demethylase 5A (KDM5A(aa 1-588)ΔAP)
  • Lysine-specific demethylase 5A (KDM5A(aa 1-739)ΔAP(2C-2S))
  • Lysine-specific demethylase 5B
  • Lysine-specific demethylase 5B (KDM5B(aa 1-604)ΔAP)
  • Lysine-specific demethylase 5B (KDM5B(aa 1-755)ΔAP)
  • Lysine-specific demethylase 5C
  • Lysine-specific demethylase 5C (KDM5C(aa 1-789)ΔAP)
  • Lysine-specific demethylase 5D (KDM5D(aa 1-760)ΔAP)
  • 3-((1-(2-(4,4-difluoropiperidin-1-yl)ethyl)-5-fluoro-1H-indazol-3-yl)amino)-isonicotinic acid (N11)
  • US10040779, Example 73
  • US10336727, Example 73
  • US9617242, Example 73
20 IC50
  • ALK tyrosine kinase receptor
  • Cereblon/Histone deacetylase 6
  • Hepatocyte growth factor receptor
  • Histone deacetylase 1
  • Histone deacetylase 10
  • Histone deacetylase 11
  • Histone deacetylase 2
  • Histone deacetylase 3
  • Histone deacetylase 4
  • Histone deacetylase 5
  • Histone deacetylase 7
  • Histone deacetylase 8
  • Histone deacetylase 9
  • Mast/stem cell growth factor receptor Kit
  • Platelet-derived growth factor receptor beta
  • Proto-oncogene tyrosine-protein kinase Src
  • Proto-oncogene tyrosine-protein kinase receptor Ret
  • Tyrosine-protein kinase receptor FLT3
  • Tyrosine-protein kinase receptor UFO
  • Vascular endothelial growth factor receptor 2
  • US9186318, 9
12 IC50 8 Kd
  • Cytoplasmic tyrosine-protein kinase BMX
  • Epidermal growth factor receptor
  • Fyn/BTK
  • LCK/BTK
  • LynA/BTK
  • Receptor protein-tyrosine kinase erbB-4
  • Receptor tyrosine-protein kinase erbB-2
  • Tyrosine-protein kinase BTK
  • Tyrosine-protein kinase ITK/TSK
  • Tyrosine-protein kinase JAK3
  • Tyrosine-protein kinase TEC
  • US9199997, 9
  • US9879013, 19(2)
20 IC50
  • 72 kDa type IV collagenase
  • A disintegrin and metalloproteinase with thrombospondin motifs 4 (ADAMTS-4)
  • A disintegrin and metalloproteinase with thrombospondin motifs 5 (ADAMTS-5)
  • Collagenase 3
  • Interstitial collagenase
  • Matrix metalloproteinase 12
  • Matrix metalloproteinase 14
  • Matrix metalloproteinase-12 (MMP12)
  • Matrix metalloproteinase-14 (MMP14)
  • Matrix metalloproteinase-7 (MMP7)
  • Matrix metalloproteinase-9
  • Metalloproteinase with thrombospondin motifs 5 (ADAMTS-5)
  • Neutrophil collagenase
  • Stromelysin-1
  • US9206139, 4
20 IC50
  • 72 kDa type IV collagenase
  • A disintegrin and metalloproteinase with thrombospondin motifs 4 (ADAMTS-4)
  • A disintegrin and metalloproteinase with thrombospondin motifs 5 (ADAMTS-5)
  • Collagenase 3
  • Interstitial collagenase
  • Matrix metalloproteinase 12
  • Matrix metalloproteinase 14
  • Matrix metalloproteinase-12 (MMP12)
  • Matrix metalloproteinase-14 (MMP14)
  • Matrix metalloproteinase-7 (MMP7)
  • Matrix metalloproteinase-9
  • Metalloproteinase with thrombospondin motifs 5 (ADAMTS-5)
  • Neutrophil collagenase
  • Stromelysin-1
  • US9206139, 5
20 IC50
  • Cathepsin B
  • Cathepsin K
  • Cathepsin S
  • Procathepsin L
  • (2S)-N-(cyanomethyl)-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfon
  • (2S)-N-(cyanomethyl)-4-methyl-2-{[(1S)-2,2,2-trifluoro-1-[4-(4-methanesulfonylphenyl)phenyl]ethyl]amino}pentanamide
  • CHEMBL437501
  • L-873724
20 IC50
  • B-RAF V600E
  • C-RAF
  • RAF proto-oncogene serine/threonine-protein kinase
  • Serine/threonine-protein kinase B-raf
  • US10245267, Example 49
  • US10709712, Example 49
  • US9242969, 49
  • US9694016, 49
20 IC50
  • B-RAF V600E
  • C-RAF
  • RAF proto-oncogene serine/threonine-protein kinase
  • Serine/threonine-protein kinase B-raf
  • US10245267, Example 88
  • US10709712, Example 88
  • US9242969, 88
  • US9694016, 1170
20 IC50
  • B-RAF V600E
  • C-RAF
  • RAF proto-oncogene serine/threonine-protein kinase
  • Serine/threonine-protein kinase B-raf
  • US10245267, Example 89
  • US10709712, Example 89
  • US9242969, 89
  • US9694016, 1171
20 IC50
  • B-RAF V600E
  • C-RAF
  • RAF proto-oncogene serine/threonine-protein kinase
  • Serine/threonine-protein kinase B-raf
  • US10245267, Example 90
  • US10709712, Example 90
  • US9242969, 90
  • US9694016, 1172
20 IC50
  • B-RAF V600E
  • C-RAF
  • RAF proto-oncogene serine/threonine-protein kinase
  • Serine/threonine-protein kinase B-raf
  • US10245267, Example 91
  • US10709712, Example 91
  • US9242969, 91
  • US9694016, 1173
16 IC50 4 EC50
  • B-RAF V600E
  • BRAF/CRAF
  • C-RAF
  • RAF proto-oncogene serine/threonine-protein kinase
  • Serine/threonine-protein kinase B-raf
  • US10245267, Example 131
  • US10709712, Example 131
  • US9242969, 131
  • US9694016, 131
20 IC50
  • B-RAF V600E
  • C-RAF
  • RAF proto-oncogene serine/threonine-protein kinase
  • Serine/threonine-protein kinase B-raf
  • US10245267, Example 155
  • US10709712, Example 155
  • US9242969, 155
  • US9694016, 155
20 IC50
  • B-RAF V600E
  • C-RAF
  • RAF proto-oncogene serine/threonine-protein kinase
  • Serine/threonine-protein kinase B-raf
  • US10245267, Example 156
  • US10709712, Example 235
  • US9242969, 156
  • US9694016, 235
20 IC50
  • B-RAF V600E
  • C-RAF
  • RAF proto-oncogene serine/threonine-protein kinase
  • Serine/threonine-protein kinase B-raf
  • US10245267, Example 165
  • US10709712, Example 165
  • US9242969, 165
  • US9694016, 653
20 IC50
  • B-RAF V600E
  • C-RAF
  • RAF proto-oncogene serine/threonine-protein kinase
  • Serine/threonine-protein kinase B-raf
  • US10245267, Example 651
  • US10709712, Example 166
  • US9242969, 166
  • US9694016, 651
20 IC50
  • B-RAF V600E
  • C-RAF
  • RAF proto-oncogene serine/threonine-protein kinase
  • Serine/threonine-protein kinase B-raf
  • US10245267, Example 645
  • US10709712, Example 167
  • US9242969, 167
  • US9694016, 645
20 IC50
  • B-RAF V600E
  • C-RAF
  • RAF proto-oncogene serine/threonine-protein kinase
  • Serine/threonine-protein kinase B-raf
  • US10245267, Example 168
  • US10709712, Example 168
  • US9242969, 168
  • US9694016, 658
6 IC50 14 Kd
  • BET bromodomain 2(1) (BRD2(1))
  • BET bromodomain 2(1,2) (BRD2(1,2))
  • BET bromodomain 2(2) (BRD2(2))
  • BET bromodomain 3(1) (BRD3(1))
  • BET bromodomain 3(1,2) (BRD3(1,2))
  • BET bromodomain 3(2) (BRD3(2))
  • BET bromodomain 4 (BRD4)
  • BET bromodomain 4(1,2) (BRD4(1,2))
  • Bromodomain testis (1, 2) (BRDT(1,2))
  • Bromodomain testis 1 (BRDT(1))
  • Bromodomain testis 2 (BRDT(2))
  • Bromodomain-containing protein 4
  • Bromodomain-containing protein 4 (BRD4)
  • Bromodomain-containing protein 4 (BRD4) (aa 44-168)
  • Bromodomain-containing protein 4 Bromo 1 domain(BRD4 BD1)
  • Bromodomain-containing protein 4 Bromo 2 domain(BRD4 BD2)
  • (R)-JQ1 (3)
  • US10407441, Compound (R)-JQ1
  • US9320741, (R)-JQ1
20 IC50
  • Transient receptor potential cation channel subfamily V member 1
  • Vanilloid receptor
  • AMG 517
  • CHEMBL229430
  • JMC503515 Compound 23
  • N-[4-({6-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl}oxy)-1,3-benzothiazol-2-yl]acetamide
  • US8796328, A
  • US8802711, H
20 IC50
  • Acetyl-CoA carboxylase 1
  • Acetyl-CoA carboxylase 2
  • US9278925, 1-1
1 Ki 10 Kd
0 ΔG°
  • Ephrin receptor
  • Ephrin type-A receptor 3 ligand binding domain (EphA3-LBD)
  • Ephrin type-A receptor 4 ligand binding domain (D61G/E62G-EphA4-LBD)
  • Ephrin type-A receptor 4 ligand binding domain (EphA4-LBD)
  • Ephrin type-A receptor 4 ligand binding domain (I159A-EphA4-LBD)
  • Ephrin type-A receptor 4 ligand binding domain (I59A-EphA4-LBD)
  • Ephrin type-A receptor 4 ligand binding domain (I59G-EphA4-LBD)
  • Ephrin type-A receptor 4 ligand binding domain (I67A-EphA4-LBD)
  • Ephrin type-A receptor 4 ligand binding domain (M164A-EphA4-LBD)
  • Ephrin type-A receptor 4 ligand binding domain (M60A-EphA4-LBD)
  • 123C4
20 IC50
  • 1,3-beta-glucan synthase component GLS2
  • Beta-secretase 1
  • Beta-secretase 1 (BACE1)
  • Beta-secretase 2
  • Cathepsin D
  • Cytochrome P450 2D6 (2D6)
  • Potassium voltage-gated channel subfamily H member 2
  • US9315520, 1
  • US9315520, Comparator 1
  • US9315520, Example 1
  • US9315520, Example 2
  • US9605007, Example 1
1 Ki 19 EC50
  • Free fatty acid receptor 1
  • Free fatty acid receptor 4
  • G-protein coupled receptor 120
  • 3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propanoic acid
  • CHEMBL207881
  • carboxylic acid agonist, 2
20 IC50
  • Tyrosine-protein kinase BTK
  • Tyrosine-protein kinase JAK2
  • US10106559, Example 14
  • US10435415, Example 14
  • US9334290, 13
  • US9334290, 14
  • US9850258, Example 14
2 Ki 11 IC50 1 EC50
0 ΔG°
  • Alpha-chymotrypsin
  • Beta-lactamase
  • Epidermal growth factor receptor
  • Glucose Transporter 1 (hGLUT1)
  • Monocarboxylate transporter 1 (MCT1)
  • Monocarboxylate transporter 2
  • Monocarboxylate transporter 4
  • Pancreatic triacylglycerol lipase
  • Serine/threonine-protein kinase 33
  • Sodium/glucose cotransporter 1 (SGLT1)
  • Sodium/glucose cotransporter 2
  • Solute carrier family 28 member 3
  • Topoisomerase I/II
  • Transcriptional Regulator TtgR
  • Transcriptional Regulator TtgR Mutant R176G
  • Transcriptional Regulator TtgR-DNA
  • 3-(4-hydroxyphenyl)-1-(2,4,6-trihydroxyphenyl)propan-1-one
  • CHEMBL45068
  • Phloretin
  • cid_4788
20 EC50
  • Serine protease NS3-NS5B
  • Serine protease NS3/RNA-directed RNA polymerase NS5B (NS3-NS5B)
  • Serine protease NS5A (L28T)
  • Serine protease NS5A (L31F)
  • Serine protease NS5A (L31M)
  • Serine protease NS5A (L31V)
  • Serine protease NS5A (R30H)
  • Serine protease NS5A (Y93C)
  • Serine protease NS5A (Y93H)
  • US9427428, 3
  • US9433609, 3
20 EC50
  • Serine protease NS3-NS5B
  • Serine protease NS3/RNA-directed RNA polymerase NS5B (NS3-NS5B)
  • Serine protease NS5A (L28T)
  • Serine protease NS5A (L31F)
  • Serine protease NS5A (L31M)
  • Serine protease NS5A (L31V)
  • Serine protease NS5A (R30H)
  • Serine protease NS5A (Y93C)
  • Serine protease NS5A (Y93H)
  • US9427428, 8
  • US9433609, 8
20 IC50
  • Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
  • Tyrosine-protein kinase JAK1
  • Tyrosine-protein kinase Mer
  • Tyrosine-protein kinase receptor TYRO3
  • Tyrosine-protein kinase receptor UFO
  • 3-(1- [1,3]oxazolo[5,4- b]pyridin-2- ylpyrrolidin-3-yl)-3- [4-(7H-pyrrolo[2,3- d]pyrimidin-4-yl)- 1H-pyrazol-1- yl]propanenitrile
  • US10053465, 4
  • US10065963, Compound 4
  • US10125150, Example 4
  • US10336759, # 4
  • US10479803, Example 4
  • US10519163, Example 4
  • US10675284, Example 4
  • US9732097, Example 4
20 IC50
  • Tyrosine-protein kinase JAK1
  • Tyrosine-protein kinase Mer
  • Tyrosine-protein kinase receptor TYRO3
  • Tyrosine-protein kinase receptor UFO
  • US10005788, 1 (2nd peak, cis-)
  • US10053465, 22
  • US10065963, Compound 22
  • US10125150, Example 22
  • US10336759, # 22
  • US10479803, Example 22
  • US10519163, Example 22
  • US10675284, Example 22
  • US9732097, Example 22
  • {1-(cis-4-{[4-{[(3S)- 3-hydroxypyrrolidin- 1-yl]methyl}-6- (trifluoromethyl) pyridin-2- yl]oxy}cyclohexyl)- 3-[4-(7H-pyrrolo[2,3- d]pyrimidin-4-yl)- 1H-pyrazol-1- yl]azetidin-3- yl jacetonitrile
20 IC50
  • Epidermal growth factor receptor
  • Tyrosine-protein kinase BTK
  • US10005782, Compound 29b
  • US9447106, 119
  • US9447106, 29
  • US9556188, Compound 29
18 IC50 2 EC50
  • CDK2/CycE
  • CDK2/Cyclin A1
  • CDK6/CycD3
  • Cyclin-Dependent Kinase 2 (CDK2)
  • Cyclin-Dependent Kinase 4 (CDK4)
  • US10189849, Compound 27
  • US9464092, T
  • US9527857, T
  • US9957276, Compound 27
10 Ki 10 IC50
  • P2X purinoceptor 7
  • P2X purinoceptor 7 (P2X7)
  • US10112937, Example 64
  • US10150765, Example 64
  • US10703749, Example 64
  • US9464084, 64
10 Ki 10 IC50
  • P2X purinoceptor 7
  • P2X purinoceptor 7 (P2X7)
  • US10112937, Example 73
  • US10150765, Example 73
  • US10703749, Example 73
  • US9464084, 73
10 Ki 10 IC50
  • P2X purinoceptor 7
  • P2X purinoceptor 7 (P2X7)
  • US10112937, Example 75
  • US10150765, Example 75
  • US10703749, Example 75
  • US9464084, 75
10 Ki 10 IC50
  • P2X purinoceptor 7
  • P2X purinoceptor 7 (P2X7)
  • US10112937, Example 87
  • US10150765, Example 87
  • US10703749, Example 87
  • US9464084, 87
10 Ki 10 IC50
  • P2X purinoceptor 7
  • P2X purinoceptor 7 (P2X7)
  • US10112937, Example 91
  • US10150765, Example 91
  • US10703749, Example 91
  • US9464084, 91
10 Ki 10 IC50
  • P2X purinoceptor 7
  • P2X purinoceptor 7 (P2X7)
  • US10112937, Example 99
  • US10150765, Example 99
  • US10703749, Example 99
  • US9464084, 99
10 Ki 10 IC50
  • P2X purinoceptor 7
  • P2X purinoceptor 7 (P2X7)
  • US10112937, Example 119
  • US10150765, Example 119
  • US10703749, Example 119
  • US9464084, 119
10 Ki 10 IC50
  • P2X purinoceptor 7
  • P2X purinoceptor 7 (P2X7)
  • US10112937, Example 133
  • US10150765, Example 133
  • US10703749, Example 133
  • US9464084, 133
10 Ki 10 IC50
  • P2X purinoceptor 7
  • P2X purinoceptor 7 (P2X7)
  • US10112937, Example 170
  • US10150765, Example 170
  • US10703749, Example 170
  • US9464084, 170
10 Ki 10 IC50
  • P2X purinoceptor 7
  • P2X purinoceptor 7 (P2X7)
  • US10112937, Example 172
  • US10150765, Example 172
  • US10703749, Example 172
  • US9464084, 172
10 Ki 10 IC50
  • P2X purinoceptor 7
  • P2X purinoceptor 7 (P2X7)
  • US10112937, Example 249
  • US10150765, Example 249
  • US10703749, Example 249
  • US9464084, 249
17 IC50 3 Kd
  • Glycogen synthase kinase-3
  • Mitogen-activated protein kinase 14
  • Potassium voltage-gated channel subfamily H member 2
  • Proto-oncogene tyrosine-protein kinase Src
  • Tyrosine-protein kinase Lck
  • Tyrosine-protein kinase SYK
  • US10125100, Example 1
  • US10392346, Example 1
  • US9499486, 1
  • US9751837, Example 1
20 IC50
  • Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
  • p110delta/p85alpha
  • 5-{3-[1-(4-Amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-methoxy-6-methylphenyl}-N,N-dimethylpyridine-2-carboxamide bis(trifluoroacetate)
  • US10092570, Example 11
  • US10376513, Example 167
  • US10646492, Example 167
  • US9707233, 11
  • US9707233, 167
  • US9707233, 41
  • US9707233, 42
  • US9707233, 66
  • US9730939, Example 167
  • US9932341, Example 167
9 Ki 10 IC50 1 Kd
  • Amine oxidase (flavin-containing) A
  • Amine oxidase [flavin-containing] B
  • GST-Lysine-specific histone demethylase 1A (LSD1)
  • Lysine-specific histone demethylase 1A
  • US10329256, Example 3
  • US9487512, 3
  • US9944601, Example 3
18 IC50 1 Kd
0 ΔG°
  • CDK2/CycE
  • Calcium/calmodulin-dependent protein kinase type II subunit delta
  • Cyclic AMP-dependent protein kinase (PKA)
  • Cyclin B/Cyclin-Dependent Kinase 1 (CDK1)/G2/mitotic-specific cyclin B2/G2/mitotic-specific cyclin B3
  • Cyclin-Dependent Kinase 4 (CDK4)
  • Epidermal growth factor receptor
  • NAD-dependent deacetylase sirtuin 2
  • PKC alpha and beta-2
  • Phosphorylase Kinase
  • Protein Kinase C
  • Protein kinase C alpha type
  • Protein kinase C, epsilon
  • Serine/threonine-protein kinase PIM
  • Serine/threonine-protein kinase pim-1
  • Tyrosine-protein kinase ABL
  • cAMP-Dependent Protein Kinase (PKA)
  • 3,4-Bis(3-indolyl)-1H-pyrrole-2,5-dione
  • 3,4-bis(1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione
  • BIM-4
  • Bisindolyl deriv. 3
  • Bisindolylmaleimide deriv. 5
  • CHEMBL266487
  • bis-indolylmaleimide deriv. 8a
13 Ki 5 IC50 2 EC50
  • Bile salt export pump
  • Canalicular multispecific organic anion transporter 2
  • Carbonic Anhydrase III
  • Carbonic Anhydrase VA
  • Carbonic Anhydrase VB
  • Carbonic Anhydrase XIII
  • Carbonic Anhydrase XIV
  • Carbonic anhydrase 1
  • Carbonic anhydrase 12
  • Carbonic anhydrase 2
  • Carbonic anhydrase 4
  • Carbonic anhydrase 6 (CA-VI)
  • Carbonic anhydrase 7
  • Carbonic anhydrase 9
  • Multidrug resistance-associated protein 4
  • Solute carrier family 22 member 6
  • electroneutral potassium-chloride cotransporter KCC2
  • 3-(butylamino)-4-phenoxy-5-sulfamoylbenzoic acid
  • Bumetanide
  • Bumex
  • Burinex
  • Fordiuran
  • cid_2471
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 6′-(5-amino-2-methylphenyl)-2′-(2,6-difluoro-3,5-dimethoxyphenyl)-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-3′(2′H)-one
  • US10251892, Example 1
  • US10632126, Example 1
  • US9708318, 1
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 6′-(5-amino-4-fluoro-2-methylphenyl)-2′-(2,6-difluoro-3,5-dimethoxyphenyl)-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-3′(2′H)-one
  • US10251892, Example 2
  • US10632126, Example 2
  • US9708318, 2
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 6′-(5-aminopyridin-3-yl)-2′-(2,6-difluoro-3,5-dimethoxyphenyl)-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-3′(2′H)-one
  • US10251892, Example 4
  • US10632126, Example 4
  • US9708318, 4
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 2′-(2,6-difluoro-3,5-dimethoxyphenyl)-6′-(5-fluoropyridin-3-yl)-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-3′(2′H)-one
  • US10251892, Example 5
  • US10632126, Example 5
  • US9708318, 5
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 2′-(2,6-difluoro-3,5-dimethoxyphenyl)-6′-(5-morpholinopyridin-3-yl)-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-3′(2′H)-one
  • US10251892, Example 6
  • US10632126, Example 6
  • US9708318, 6
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 6′-(5-amino-2-methylpyridin-3-yl)-2′-(2,6-difluoro-3,5-dimethoxyphenyl)-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-3′(2′H)-one
  • US10251892, Example 7
  • US10632126, Example 7
  • US9708318, 7
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 5-(2′-(2,6-difluoro-3,5-dimethoxyphenyl)-3′-oxo-2′,3′-dihydro-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridine]-6′-yl)nicotinonitrile
  • US10251892, Example 8
  • US10632126, Example 8
  • US9708318, 8
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 2′-(2,6-difluoro-3,5-dimethoxyphenyl)-6′-(pyridin-3-yl)-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-3′(2′H)-one
  • US10251892, Example 9
  • US10632126, Example 9
  • US9708318, 9
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 2′-(2,6-difluoro-3,5-dimethoxyphenyl)-6′-(5-methoxypyridin-3-yl)-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-3′(2′H)-one
  • US10251892, Example 10
  • US10632126, Example 10
  • US9708318, 10
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 6′-(5-chloropyridin-3-yl)-2′-(2,6-difluoro-3,5-dimethoxyphenyl)-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-3′(2′H)-one
  • US10251892, Example 11
  • US10632126, Example 11
  • US9708318, 11
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 6′-(5-(1H-imidazol-1-yl)pyridin-3-yl)-2′-(2,6-difluoro-3,5-dimethoxyphenyl)-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-3′(2′H)-one
  • US10251892, Example 12
  • US10632126, Example 12
  • US9708318, 12
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 2′-(2,6-difluoro-3,5-dimethoxyphenyl)-6′-(5-(morpholine-4-carbonyl)pyridin-3-yl)-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-3′(2′H)-one
  • US10251892, Example 13
  • US10632126, Example 13
  • US9708318, 13
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 2′-(2,6-difluoro-3,5-dimethoxyphenyl)-6′-(5-(morpholinosulfonyl)pyridin-3-yl)-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-3′(2′H)-one
  • US10251892, Example 14
  • US10632126, Example 14
  • US9708318, 14
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • N-(5-(2′-(2,6-difluoro-3,5-dimethoxyphenyl)-3′-oxo-2′,3′-dihydro-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridine]-6′-yl)pyridin-3-yl)methanesulfonamide
  • US10251892, Example 15
  • US10632126, Example 15
  • US9708318, 15
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 2′-(2,6-difluoro-3,5-dimethoxyphenyl)-6′-(5-(morpholinomethyl)pyridin-3-yl)-1′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-3′(2′H)-one
  • US10251892, Example 16
  • US10632126, Example 16
  • US9708318, 16
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • US10251892, Example 57
  • US10632126, Example 57
  • US9708318, 57
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 3-(2,6-difluoro-3,5- dimethoxyphenyl)-7-(1,3- dimethyl-1H-pyrazol-4-yl)-1- ((2-methoxypyridin-4- yl)methyl)-3,4- dihydropyrido[4,3-d]pyrimidin- 2(1H)-one
  • US10251892, Example 58
  • US10632126, Example 58
  • US9708318, 58
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • US10251892, Example 59
  • US10632126, Example 59
  • US9708318, 59
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • US10251892, Example 69
  • US10632126, Example 69
  • US9708318, 69
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • US10251892, Example 168
  • US10632126, Example 168
  • US9708318, 168
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 3-(2,6-difluoro-3,5- dimethoxyphenyl)-1-ethyl-7-(1- methyl-1H-pyrazol-4-yl)-3,4- dihydropyrido[4,3-d]pyrimidin-2(1H)- one
  • US10251892, Example 169
  • US10632126, Example 169
  • US9708318, 169
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 3-(2,6-difluoro-3,5- dimethoxyphenyl)-7-(1,3-dimethyl- 1H-pyrazol-4-yl)-1-ethyl-3,4- dihydropyrido[4,3-d]pyrimidin-2(1H)- one
  • US10251892, Example 170
  • US10632126, Example 170
  • US9708318, 170
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 5-(3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-2-oxo-1,2,3,4-tetrahydropyrido[4,3-d]pyrimidin-7-yl)-N-ethylpicolinamide
  • US10251892, Example 175
  • US10632126, Example 175
  • US9708318, 175
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 2′-(2,6-difluoro-3,5-dimethoxyphenyl)-6′-(1-methyl-1H-pyrazol-4-yl)-1′,2′-dihydro-3′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-3′-one
  • US10251892, Example 186
  • US10632126, Example 186
  • US9708318, 186
20 IC50
  • Fibroblast growth factor receptor 1
  • Fibroblast growth factor receptor 2
  • Fibroblast growth factor receptor 3
  • Fibroblast growth factor receptor 4
  • 1-(5-{3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-[(5-methyl-1,3,4-oxadiazol-2-yl)methyl]-2-oxo-1,2,3,4-tetrahydropyrido[4,3-d]pyrimidin-7-yl}pyridin-2-yl)cyclobutanecarbonitrile
  • US10251892, Example 187
  • US10632126, Example 187
  • US9708318, 187
20 IC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4A
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5B
  • jmjd2a
  • 2-(3-cyclopropyl-5-hydroxy-1H- pyrazol-1-yl)isonicotinic acid
  • US10173996, Example 2
  • US9604961, Example 2
  • US9714230, 2
  • US9908865, Example 2
19 IC50 1 EC50
  • Lysine-specific demethylase 4A
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5A/5B
  • Lysine-specific demethylase 5B
  • jmjd2a
  • 2-(5-(benzyloxy)-1H-pyrazol-1- yl)isonicotinic acid
  • US10173996, Example 39
  • US9604961, Example 39
  • US9714230, 39
  • US9908865, Example 39
19 IC50 1 EC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5A/5B
  • Lysine-specific demethylase 5B
  • 2-{5-[(4-fluorobenzyl)oxy]-1H- pyrazol-1-yl}pyridine-4- carboxylic acid
  • US10173996, Example 40
  • US9604961, Example 40
  • US9714230, 40
  • US9908865, Example 40
19 IC50 1 EC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5A/5B
  • Lysine-specific demethylase 5B
  • 2-{5-[(4-methylbenzyl)oxy]-1H- pyrazol-1-yl}pyridine-4- carboxylic acid
  • US10173996, Example 55
  • US9604961, Example 55
  • US9714230, 55
  • US9908865, Example 55
19 IC50 1 EC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5A/5B
  • Lysine-specific demethylase 5B
  • 2-{5-[(4-ethylbenzyl)oxy]- 1H-pyrazol-1-yl}pyridine- 4-carboxylic acid
  • US10173996, Example 56
  • US9604961, Example 56
  • US9714230, 56
  • US9908865, Example 56
19 IC50 1 EC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5A/5B
  • Lysine-specific demethylase 5B
  • 2-[5-[(4- cyanophenyl)methoxy]pyrazol-1- yl]pyridine-4-carboxylic acid
  • US10173996, Example 99
  • US9604961, Example 99
  • US9714230, 99
  • US9908865, Example 99
19 IC50 1 EC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5A/5B
  • Lysine-specific demethylase 5B
  • 2-[5-[(4-chloro-2- phenylmethoxyphenyl)methoxy] pyrazol-1-yl]pyridine-4-carboxylic acid
  • US10173996, Example 105
  • US9604961, Example 105
  • US9714230, 105
  • US9908865, Example 105
20 IC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4A
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5B
  • jmjd2a
  • 2-[5-[(2-butoxy-4- chlorophenyl)methoxy]pyrazol-1- yl]pyridine-4-carboxylic acid
  • US10173996, Example 111
  • US9604961, Example 111
  • US9714230, 111
  • US9908865, Example 111
20 IC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4A
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5B
  • jmjd2a
  • 2-[5-[[4-chloro-2-(2- methylpropoxy)phenyl]methoxy] pyrazol-1-yl]pyridine-4-carboxylic acid
  • US10173996, Example 112
  • US9604961, Example 112
  • US9714230, 112
  • US9908865, Example 112
20 IC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4A
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5B
  • jmjd2a
  • 2-[5-[[4-chloro-2-[(4- fluorophenyl)methoxy]phenyl] methoxy]pyrazol-1-yl]pyridine- 4-carboxylic acid
  • US10173996, Example 117
  • US9604961, Example 117
  • US9714230, 117
  • US9908865, Example 117
20 IC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4A
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5B
  • jmjd2a
  • 2-[5-[[4-fluoro-2-[(4- fluorophenyl)methoxy]phenyl] methoxy]pyrazol-1-yl]pyridine- 4-carboxylic acid
  • US10173996, Example 118
  • US9604961, Example 118
  • US9714230, 118
  • US9908865, Example 118
20 IC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4A
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5B
  • jmjd2a
  • 2-[5-[(2-chloro-4- methylphenyl)methoxy]pyrazol-1- yl]pyridine-4-carboxylic acid
  • US10173996, Example 130
  • US9604961, Example 130
  • US9714230, 130
  • US9908865, Example 130
20 IC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4A
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5B
  • jmjd2a
  • 2-[5-[(2,4- dimethylphenyl)methoxy]pyrazol- 1-yl]pyridine-4-carboxylic acid
  • US10173996, Example 132
  • US9604961, Example 132
  • US9714230, 132
  • US9908865, Example 132
20 IC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4A
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5B
  • jmjd2a
  • 2-[5-[(2-methoxy-4- methylphenyl)methoxy]pyrazol-1- yl]pyridine-4-carboxylic acid
  • US10173996, Example 133
  • US9604961, Example 133
  • US9714230, 133
  • US9908865, Example 133
20 IC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4A
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5B
  • jmjd2a
  • 2-[5-[[4-chloro-3- (cyclopropylmethoxy)phenyl] methoxy]pyrazol-1-yl]pyridine- 4-carboxylic acid
  • US10173996, Example 140
  • US9604961, Example 140
  • US9714230, 140
  • US9908865, Example 140
20 IC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4A
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5B
  • jmjd2a
  • 2-[3-(4-chlorophenyl)-5- hydroxypyrazol-1-yl]pyridine-4- carboxylic acid
  • US10173996, Example 158
  • US9604961, Example 158
  • US9714230, 158
  • US9908865, Example 158
20 IC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4A
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5B
  • jmjd2a
  • 2-[3-(3-chlorophenyl)-5- hydroxypyrazol-1-yl]pyridine-4- carboxylic acid
  • US10173996, Example 159
  • US9604961, Example 159
  • US9714230, 159
  • US9908865, Example 159
20 IC50
  • Lysine-specific demethylase 2B
  • Lysine-specific demethylase 4A
  • Lysine-specific demethylase 4C
  • Lysine-specific demethylase 5A
  • Lysine-specific demethylase 5B
  • jmjd2a
  • 2-(3-cyclopentyl-5- hydroxypyrazol-1-yl)pyridine-4- carboxylic acid
  • US10173996, Example 160
  • US9604961, Example 160
  • US9714230, 160
  • US9908865, Example 160
19 IC50 1 EC50
  • Abhydrolase Domain-Containing Protein 6
  • Anandamide amidohydrolase
  • Fatty-acid amide hydrolase 1
  • KIAA1363
  • Monoglyceride Lipase (MGL)
  • Monoglyceride lipase
  • Sn1-specific diacylglycerol lipase alpha
  • Transient receptor potential cation channel subfamily A member 1
  • Transient receptor potential cation channel subfamily V member 1
  • CHEMBL509860
  • LY2183240
  • N,N-dimethyl-5-[(4-phenylphenyl)methyl]-1H-1,2,3,4-tetrazole-1-carboxamide
14 Ki 6 IC50
  • 72 kDa type IV collagenase
  • A disintegrin and metalloproteinase with thrombospondin motifs 4 (ADAMTS-4)
  • A disintegrin and metalloproteinase with thrombospondin motifs 5 (ADAMTS-5)
  • ADAM17
  • ADAMTS1
  • Collagenase 3
  • Disintegrin and metalloproteinase domain-containing protein 10 (ADAM10)
  • Disintegrin and metalloproteinase domain-containing protein 17
  • Interstitial collagenase
  • Matrix metalloproteinase 10
  • Matrix metalloproteinase 15
  • Matrix metalloproteinase 16
  • Matrix metalloproteinase-12 (MMP12)
  • Matrix metalloproteinase-14 (MMP14)
  • Matrix metalloproteinase-7 (MMP7)
  • Matrix metalloproteinase-9
  • Neutrophil collagenase
  • Stromelysin-1
  • (3R,4R)-3-N-hydroxy-4-N-(4-{[2-(trifluoromethyl)-1H-1,3-benzodiazol-1-yl]methyl}benzene)oxane-3,4-diamido
  • CHEMBL253275
  • benzimidazole analog., 32
4 Ki 16 IC50
  • Poly [ADP-ribose] polymerase 1
  • Poly [ADP-ribose] polymerase-1
  • poly-ADP-ribose polymerase 2 (PARP2)
  • 3-AB
  • 3-aminobenzamide
  • CHEMBL81977
2 Ki 17 IC50 1 EC50
  • 1,3-beta-glucan synthase component GLS2
  • ALK5
  • Cytochrome P450 1A
  • Cytochrome P450 2C19
  • Cytochrome P450 2C8
  • Cytochrome P450 2C9
  • Cytochrome P450 2D6
  • Cytochrome P450 3A
  • Nuclear receptor subfamily 1 group I member 2
  • Phosphodiesterase 4
  • TGF-beta receptor type II
  • TGF-beta receptor type-1
  • TGF-betaR1 T204D
  • 6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-1H- imidazol-5-yl)imidazo[1,2-b]pyridazine-3-carbonitrile
  • US10287295, Example 32'
  • US9884868, Example 32'
20 IC50
  • 3',5'-cyclic phosphodiesterase
  • Homo sapiens phosphodiesterase 2A (PDE2A)
  • cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
  • US10023575, Example 46
  • US10023575, Example 47
  • US10023575, Example 81a
  • US10023575, Example 81b
  • US10479794, Example 81b
  • US10875867, Example 47
20 IC50
  • 3',5'-cyclic phosphodiesterase
  • Homo sapiens phosphodiesterase 2A (PDE2A)
  • cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
  • US10023575, Example 48
  • US10023575, Example 49
  • US10023575, Example 82a
  • US10023575, Example 82b
  • US10479794, Example 82b
  • US10875867, Example 49
20 Kd
  • Peptidyl-prolyl cis-trans isomerase FKBP1B/Serine/threonine-protein kinase mTOR
  • Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
  • Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
  • Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha
  • Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta
  • US10087187, Compound 14
  • US10087187, Compound 14a
  • US10087187, Compound 14b
  • US10087187, Compound 14c
20 Ki
  • Non-receptor tyrosine-protein kinase TYK2
  • Tyrosine-protein kinase JAK1
  • Tyrosine-protein kinase JAK2
  • Tyrosine-protein kinase JAK3
  • US10100049, Example 2
  • US10183942, Example 2-3
  • US10526330, Example 2
20 Ki
  • Non-receptor tyrosine-protein kinase TYK2
  • Tyrosine-protein kinase JAK1
  • Tyrosine-protein kinase JAK2
  • Tyrosine-protein kinase JAK3
  • US10100049, Example 7
  • US10183942, Example 7-3
  • US10526330, Example 7
20 Ki
  • Non-receptor tyrosine-protein kinase TYK2
  • Tyrosine-protein kinase JAK1
  • Tyrosine-protein kinase JAK2
  • Tyrosine-protein kinase JAK3
  • US10100049, Example 14
  • US10183942, Example 14-7
  • US10526330, Example 14
13 IC50 2 Kd 5 EC50
  • Androgen Receptor
  • Androgen receptor
  • Baculoviral IAP repeat-containing protein 2/Estrogen receptor
  • Estradiol receptor beta (ERβ)
  • Estrogen receptor
  • Estrogen-Related Receptor, gamma
  • Estrogen-related receptor gamma
  • GTP-binding protein Rheb
  • GTPase KRas
  • Sarcoplasmic/endoplasmic reticulum calcium ATP-ase
  • Sarcoplasmic/endoplasmic reticulum calcium ATPase 2
  • Bisphenol A (BPA)
  • Diphenylolpropane
  • US9688816, L
20 IC50
  • Non-receptor tyrosine-protein kinase TYK2
  • Tyrosine-protein kinase JAK1
  • Tyrosine-protein kinase JAK2
  • Tyrosine-protein kinase JAK3
  • (1s,3s)-3-(Cyanomethyl)-3-(4-(6-(5-(hydroxymethyl)isoxazol-3-yl)pyrazolo[1,5-a]pyrazin-4-yl)-1H-pyrazol-1-yl)cyclobutane-1-carbonitrile (cis isomer)
  • US10144738, Example 1
  • US10144738, Example 6
  • US10822341, Example 1
20 IC50
  • Non-receptor tyrosine-protein kinase TYK2
  • Tyrosine-protein kinase JAK1
  • Tyrosine-protein kinase JAK2
  • Tyrosine-protein kinase JAK3
  • 2-(1-(Cyclopropylsulfonyl)-3-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl)-1H-pyrazol-1-yl)azetidin-3-yl)acetonitrile
  • US10144738, Example 31
  • US10144738, Example 9
  • US10822341, Example 9
18 IC50 2 EC50
  • 5-hydroxytryptamine receptor 1A
  • Apoptotic peptidase activating factor 1
  • Bcl-2-related protein A1
  • Caspase-3
  • Caspase-9
  • Dual Specificity Protein Phosphatase 1
  • MKP-3
  • MPI protein
  • SUMO-1-specific protease
  • SUMO/sentrin specific peptidase family member 8
  • diphosphomevalonate decarboxylase
  • tyrosyl-DNA phosphodiesterase 2
  • MLS000079925
  • N-[3-cyano-1-(4-methoxyphenyl)-2-pyrrolo[3,2-b]quinoxalinyl]-2-furancarboxamide
  • N-[3-cyano-1-(4-methoxyphenyl)pyrrolo[3,2-b]quinoxalin-2-yl]-2-furamide
  • N-[3-cyano-1-(4-methoxyphenyl)pyrrolo[3,2-b]quinoxalin-2-yl]furan-2-carboxamide
  • SMR000039887
  • cid_658939
19 Ki 1 EC50
  • 5-hydroxytryptamine receptor 1A
  • ADRA2C
  • Adrenergic receptor alpha-2
  • Alpha-2A adrenergic receptor
  • Alpha-2B adrenergic receptor
  • Alpha-2C adrenergic receptor
  • adrenergic Alpha2
  • Ajmalicine
  • MLS000111555
  • Raubasine
  • SMR000107477
  • cid_251561
20 Ki
  • Orexin receptor type 1
  • Orexin receptor type 1 (OX1)
  • Orexin receptor type 2
  • (R/S)-(2-(2H-1,2,3-triazol-2-yl)phenyl)(3-methyl-6-((5-(trifluoromethyl)pyridin-2-yl)oxy)-2-azabicyclo[2.2.1]heptan-2-yl)methanone
  • US9611262, Example 2
  • US9611262, Example 201
  • US9611262, Example 21
  • US9611262, Example 21A
  • US9611262, Example 21B
  • US9611262, Example 2A
  • US9611262, Example 2B
2 Ki 12 IC50 6 Kd
  • PI3-kinase class I
  • Peptidyl-prolyl cis-trans isomerase FKBP1B/Serine/threonine-protein kinase mTOR
  • Phosphatidylinositol 3-kinase catalytic subunit type 3
  • Phosphatidylinositol 3-kinase regulatory subunit beta
  • Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
  • Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform
  • Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
  • Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
  • Target of rapamycin complex 2 subunit MAPKAP1
  • Target of rapamycin complex subunit LST8
  • mTOR/FKBP12A/FKBP12B
  • US10172858, Table 1.1
  • US10172858, Table 1.22
Displayed 1 to 50 (of 134 total ) | Next | Last >>