| Id |
Subject |
Object |
Predicate |
Lexical cue |
| T139 |
0-8 |
Sentence |
denotes |
Table 2. |
| T140 |
9-40 |
Sentence |
denotes |
FDA approved kinase inhibitors: |
| T141 |
41-80 |
Sentence |
denotes |
Kinase targets and respiratory benefits |
| T142 |
81-306 |
Sentence |
denotes |
Kinase Inhibitor (brand name)(indication; main therapeutic targets) Selected Kinase Target Affinity(antiviral and pulmonary benefit)KINOMEscan(kd<100 nM) Anti-inflammatory activity, cytokine suppression, antifibrotic activity |
| T143 |
307-327 |
Sentence |
denotes |
Midostaurin (Rydapt) |
| T144 |
328-432 |
Sentence |
denotes |
(acute myeloid leukemia, systemic mastocytosis; multi-targeted; FLT3-ITD, D816V-c-KIT) AAK1, JAK2, JAK3, |
| T145 |
433-448 |
Sentence |
denotes |
Kd KIT (220nM), |
| T146 |
449-463 |
Sentence |
denotes |
Kd RET (350nM) |
| T147 |
464-517 |
Sentence |
denotes |
(48) Anti-inflammatory and cytokine suppression (107) |
| T148 |
518-530 |
Sentence |
denotes |
Lestaurtinib |
| T149 |
531-664 |
Sentence |
denotes |
(orphan drug status, acute myeloid leukemia; multi-targeted; FLT3, JAK2, TrkA, TrkB, TrkC) AAK1, AXL, FYN, GAK, JAK1, JAK2, JAK3, RET |
| T150 |
665-729 |
Sentence |
denotes |
Kd KIT (150nM)* Anti-inflammatory and cytokine suppression (107) |
| T151 |
730-752 |
Sentence |
denotes |
Gilteritinib (Xospata) |
| T152 |
753-777 |
Sentence |
denotes |
(acute myeloid leukemia; |
| T153 |
778-796 |
Sentence |
denotes |
FLT3-ITD; AXL) AXL |
| T154 |
797-809 |
Sentence |
denotes |
IC50 (41 nM) |
| T155 |
810-816 |
Sentence |
denotes |
(49)** |
| T156 |
817-836 |
Sentence |
denotes |
Dasatinib (Sprycel) |
| T157 |
837-1061 |
Sentence |
denotes |
(chronic myeloid leukemia, Ph+acute lymphoblastic leukemia; multi-targeted; BCR-ABL, SRC) ABL1, ABL2, CSK, FYN, GAK, KIT, LYN, SRC, YES Anti-inflammatory, cytokine suppression, antifibrotic (100) (99) (102) (103) (104) (101) |
| T158 |
1062-1119 |
Sentence |
denotes |
Imatinib Mesylate (Gleevec (US)/Glivec (Europe/Australia) |
| T159 |
1120-1484 |
Sentence |
denotes |
(chronic myeloid leukemia, Ph+acute lymphoblastic leukemia, gastrointestinal stromal tumor, chronic eosinophilic leukemia, hypereosinophilic syndrome, systemic mastocytosis; myelodysplastic syndrome; BCR-ABL, KIT, FIP1L1-PDGFRalpha) ABL1, ABL2, KIT Anti-inflammatory, cytokine suppression/immunomodulatory, antifibrotic (91) (92) (90) (79) (94) (95) (96) (93) (77) |
| T160 |
1485-1504 |
Sentence |
denotes |
Nilotinib (Tasigna) |
| T161 |
1505-1605 |
Sentence |
denotes |
(chronic myeloid leukemia; BCR-ABL) ABL1, ABL2, KIT Antifibrotic ((80) (81) (82) (83) (84) (85) (86) |
| T162 |
1606-1625 |
Sentence |
denotes |
Ponatinib (Iclusig) |
| T163 |
1626-1747 |
Sentence |
denotes |
(chronic myeloid leukemia, Ph+ acute lymphoblastic leukemia; BCR-ABL) ABL1, ABL2, KIT, RET, SRC Cytokine suppression (78) |
| T164 |
1748-1759 |
Sentence |
denotes |
Saracatinib |
| T165 |
1760-1841 |
Sentence |
denotes |
(orphan drug status, idiopathic pulmonary fibrosis; ABL, SRC, LCK, FGR, BLK) ABL1 |
| T166 |
1842-1861 |
Sentence |
denotes |
FYN, LYN, SRC, YES1 |
| T167 |
1862-1985 |
Sentence |
denotes |
IC50 v-ABL (30 nM); IC50 FYN (10 nM); IC50 LYN (5 nM) (isolated protein kinase assay) (186)** Antifibrotic (100) (99) (105) |
| T168 |
1986-2005 |
Sentence |
denotes |
Bosutinib (Bosulif) |
| T169 |
2006-2168 |
Sentence |
denotes |
(chronic myeloid leukemia; ABL, SRC) ABL1, ABL2, AXL, CSK, EGFR, FYN, GAK, LYN, SRC, YES Anti-inflammatory, cytokine suppression, and antifibrotic (104) (87) (88) |
| T170 |
2169-2191 |
Sentence |
denotes |
Baricitinib (Olumiant) |
| T171 |
2192-2243 |
Sentence |
denotes |
(rheumatoid arthritis; JAK1, JAK2) JAK1, JAK2, TYK2 |
| T172 |
2244-2362 |
Sentence |
denotes |
Kd AAK1 (17 nM); Kd GAK (136 nM) (cell-free assay) (47)** Anti-inflammatory and cytokine suppression (106) (107) (108) |
| T173 |
2363-2383 |
Sentence |
denotes |
Ruxolitinib (Jakafi) |
| T174 |
2384-2458 |
Sentence |
denotes |
(myelofibrosis, polycythemia vera; JAK1, JAK2) GAK, JAK1, JAK2, JAK3, TYK2 |
| T175 |
2459-2580 |
Sentence |
denotes |
Kd AAK1 (100 nM); Kd GAK (120 nM) (cell-free assay) (47)** Anti-inflammatory and cytokine suppression, antifibrotic (107) |
| T176 |
2581-2601 |
Sentence |
denotes |
Fedratinib (Inrebic) |
| T177 |
2602-2655 |
Sentence |
denotes |
(myelofibrosis; JAK2) AAK1, ABL1, FYN, GAK, JAK2, SRC |
| T178 |
2656-2763 |
Sentence |
denotes |
Kd AAK1 32 nM; Kd GAK 1 nM (cell-free assay) (47)** Anti-inflammatory and cytokine suppression, (107) (115) |
| T179 |
2764-2788 |
Sentence |
denotes |
Tofacitinib (XELJANZ XR) |
| T180 |
2789-2911 |
Sentence |
denotes |
(ulcerative colitis, rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis; JAK1, JAK3) JAK1, JAK2, JAK3, TYK2 |
| T181 |
2912-3011 |
Sentence |
denotes |
No AAK1 inhibitory activity (47) Anti-inflammatory and cytokine suppression (109) (110) (107) (111) |
| T182 |
3012-3030 |
Sentence |
denotes |
Gefitinib (Iressa) |
| T183 |
3031-3112 |
Sentence |
denotes |
(non-small cell lung cancer; EGFR) EGFR, GAK Antifibrotic (119) (116) (178) (118) |
| T184 |
3113-3132 |
Sentence |
denotes |
Afatinib (Gilotrif) |
| T185 |
3133-3266 |
Sentence |
denotes |
(non-small cell lung cancer, advanced squamous cell carcinoma; Her2/EGFR) EGFR, GAK Anti-inflammatory, antifibrotic (116) (178) (179) |
| T186 |
3267-3296 |
Sentence |
denotes |
Lapatinib (Tykerb and Tyverb) |
| T187 |
3297-3359 |
Sentence |
denotes |
(breast cancer; Erb1/Erb2, EGFR) EGFR Antifibrotic (116) (178) |
| T188 |
3360-3383 |
Sentence |
denotes |
Osimertinib (Tagrisso)’ |
| T189 |
3384-3423 |
Sentence |
denotes |
(non-small cell lung cancer; EGFR) EGFR |
| T190 |
3424-3551 |
Sentence |
denotes |
(60)** AZ5104, active metabolite of osimertinib, downregulates Th17-related cytokine production via inhibition of SRC-ERK-STAT3 |
| T191 |
3552-3557 |
Sentence |
denotes |
(127) |
| T192 |
3558-3577 |
Sentence |
denotes |
Erlotinib (Tarceva) |
| T193 |
3578-3647 |
Sentence |
denotes |
(non-small cell lung cancer, pancreatic cancer; Erb1, EGFR) EGFR, GAK |
| T194 |
3648-3663 |
Sentence |
denotes |
Kd ABL1 (310nM) |
| T195 |
3664-3693 |
Sentence |
denotes |
(48) Antifibrotic (116) (178) |
| T196 |
3694-3713 |
Sentence |
denotes |
Neratinib (Nerlynx) |
| T197 |
3714-3745 |
Sentence |
denotes |
(breast cancer; Her2/EGFR) EGFR |
| T198 |
3746-3766 |
Sentence |
denotes |
Pazopanib (Votrient) |
| T199 |
3767-3908 |
Sentence |
denotes |
(renal cell carcinoma, advanced soft tissue sarcoma; multi-targeted; c-KIT, FGFR, PDGFR, VEGFR) KIT Anti-inflammatory potential, antifibrotic |
| T200 |
3909-3914 |
Sentence |
denotes |
(136) |
| T201 |
3915-3934 |
Sentence |
denotes |
Sorafenib (Nexavar) |
| T202 |
3935-4074 |
Sentence |
denotes |
(renal cell carcinoma, hepatocellular carcinoma, thyroid cancer; multi-targeted; PDGFR, VEGFR, RAF) KIT, RET Antifibrotic (125) (126) (187) |
| T203 |
4075-4100 |
Sentence |
denotes |
Sunitinib malate (Sutent) |
| T204 |
4101-4298 |
Sentence |
denotes |
(renal cell carcinoma, gastrointestinal stromal tumor; multi-targeted; PDGFR, VEGFR) AAK1, AXL, GAK, JAK1, KIT, RET Anti-inflammatory potential, cytokine suppression, antifibrotic (137) (135) (107) |
| T205 |
4299-4316 |
Sentence |
denotes |
Axitinib (Inlyta) |
| T206 |
4317-4442 |
Sentence |
denotes |
(renal cell carcinoma; c-KIT, PDGFR, VEGFR1, VEGFR2, VEGFR3) ABL1, ABL2, KIT Anti-inflammatory and cytokine suppression (128) |
| T207 |
4443-4464 |
Sentence |
denotes |
Vandetanib (Caprelsa) |
| T208 |
4465-4538 |
Sentence |
denotes |
(medullary thyroid carcinoma; EGFR, RET, VEGFR) ABL2, EGFR, GAK, RET, SRC |
| T209 |
4539-4559 |
Sentence |
denotes |
Kd ABL1 (270nM) (48) |
| T210 |
4560-4582 |
Sentence |
denotes |
Regorafenib (Stivarga) |
| T211 |
4583-4699 |
Sentence |
denotes |
(colorectal cancer, gastrointestinal stromal tumor, hepatocellular cancer; PDGFRβ, Raf-1, TIE2, VEGFR1/2/3) KIT, RET |
| T212 |
4700-4721 |
Sentence |
denotes |
Ibrutinib (Imbruvica) |
| T213 |
4722-4902 |
Sentence |
denotes |
(mantel cell lymphoma, Waldenstrom macroglobulinemia, chronic lymphocytic leukemia, Small lymphocytic lymphoma, marginal zone lymphoma; BTK) EGFR, RET Anti-inflammatory (132) (133) |
| T214 |
4903-4924 |
Sentence |
denotes |
Palbociclib (Ibrance) |
| T215 |
4925-4957 |
Sentence |
denotes |
(breast cancer; CDK4, CDK6) CDK6 |
| T216 |
4958-4994 |
Sentence |
denotes |
Abemaciclib (Verzenio and Verzenios) |
| T217 |
4995-5026 |
Sentence |
denotes |
(breast cancer, CDK4,CDK6) CDK6 |
| T218 |
5027-5043 |
Sentence |
denotes |
IC50 (10 nmol/L) |
| T219 |
5044-5048 |
Sentence |
denotes |
CDK9 |
| T220 |
5049-5065 |
Sentence |
denotes |
IC50 (57 nmol/L) |
| T221 |
5066-5175 |
Sentence |
denotes |
(188)** Abemaciclib in combination with anastrozole led to increased cytokine signaling and immune activation |
| T222 |
5176-5181 |
Sentence |
denotes |
(189) |
| T223 |
5182-5191 |
Sentence |
denotes |
Alvocidib |
| T224 |
5192-5289 |
Sentence |
denotes |
(orphan drug status, acute myeloid leukemia; CDK1, CDK2, CDK4, CDK9) CDK9 Anti-inflammatory (134) |
| T225 |
5290-5309 |
Sentence |
denotes |
Ceritinib (Zykadia) |
| T226 |
5310-5364 |
Sentence |
denotes |
(non-small cell lung cancer; ALK, IGF1R, InsR, STK22D) |
| T227 |
5365-5385 |
Sentence |
denotes |
Crizotinib (Xalkori) |
| T228 |
5386-5434 |
Sentence |
denotes |
(non-small cell lung cancer; ALK/ROS1) ABL1, AXL |
| T229 |
5435-5454 |
Sentence |
denotes |
Masitinib (Masivet) |
| T230 |
5455-5561 |
Sentence |
denotes |
(orphan drug status, potential amyotrophic lateral sclerosis drug; FAK, FGFR3, KIT, LCK, PDGFR) ABL1, KIT, |
| T231 |
5562-5565 |
Sentence |
denotes |
LYN |
| T232 |
5566-5596 |
Sentence |
denotes |
Nintedanib (Ofev and Vargatef) |
| T233 |
5597-5792 |
Sentence |
denotes |
(idiopathic pulmonary fibrosis, non-small cell lung cancer; FGFR, PDGFR, VEGFR) AAK1, ABL1, AXL, JAK2, JAK3, KIT, RET, YES1 Anti-inflammatory, cytokine suppression, antifibrotic (129) (130) (131) |
| T234 |
5793-5805 |
Sentence |
denotes |
Left Column: |
| T235 |
5806-5870 |
Sentence |
denotes |
Drug names and disease indication, and main therapeutic targets. |
| T236 |
5871-5885 |
Sentence |
denotes |
Middle Column: |
| T237 |
5886-6146 |
Sentence |
denotes |
Potency (based on KINOMEscan data) against key proteins associated with respiratory function and proteins involved in viral replication/life span/infection- believed to be necessary for a wide variety of viruses, including SARS-CoV and MERS-CoV and SARS-CoV-2. |
| T238 |
6147-6160 |
Sentence |
denotes |
Right column: |
| T239 |
6161-6262 |
Sentence |
denotes |
Anti-inflammatory activity, cytokine suppression, and antifibrotic activity of the kinase inhibitors. |
| T240 |
6263-6342 |
Sentence |
denotes |
*These values were derived from ChEMBL database: https://www.ebi.ac.uk/chembl/. |
| T241 |
6343-6413 |
Sentence |
denotes |
**These values were not derived from KINOMEscan; References are cited. |
