Page last updated: 2024-11-13
azd4547
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 51039095 |
| CHEBI ID | 63453 |
| SCHEMBL ID | 63884 |
| SCHEMBL ID | 15250892 |
| MeSH ID | M0574060 |
Synonyms (55)
| Synonym |
|---|
| BCP9000364 |
| AZD4547 , |
| azd-4547 |
| azd 4547 |
| HY-13330 |
| CS-0971 |
| 1035270-39-3 |
| NCGC00346713-01 |
| n-{5-[2-(3,5-dimethoxyphenyl)ethyl]-1h-pyrazol-3-yl}-4-(cis-3,5-dimethylpiperazin-1-yl)benzamide |
| n-{5-[2-(3,5-dimethoxyphenyl)ethyl]-1h-pyrazol-3-yl}-4-[(3r,5s)-3,5-dimethylpiperazin-1-yl]benzamide |
| CHEBI:63453 , |
| 2167og1ekj , |
| unii-2167og1ekj |
| kb-74810 |
| absk091 |
| absk-091 |
| azd 4547 [who-dd] |
| benzamide, n-(5-(2-(3,5-dimethoxyphenyl)ethyl)-1h-pyrazol-3-yl)-4-((3r,5s)-3,5-dimethyl-1-piperazinyl)-, rel- |
| S2801 |
| n-(5-(3,5-dimethoxyphenethyl)-1h-pyrazol-3-yl)-4-((3s,5r)-3,5-dimethylpiperazin-1-yl)benzamide |
| rel-n-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1h-pyrazol-3-yl]-4-[(3r,5s)-3,5-dimethyl-1-piperazinyl]benzamide |
| n-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2h-pyrazol-3-yl]-4-[(3r,5s)-3,5-dimethylpiperazin-1-yl]benzamide |
| VRQMAABPASPXMW-HDICACEKSA-N |
| n-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2h-pyrazol-3-yl]-4-[(3r,5s)-3,5-dimethylpiperazin -1-yl]benzamide |
| n-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1h-pyrazol-3-yl]-4-[(3r,5s)-3,5-dimethylpiperazin-1-yl]benzamide |
| 66T , |
| gtpl7707 |
| n-{3-[2-(3,5-dimethoxyphenyl)ethyl]-1h-pyrazol-5-yl}-4-[(3r,5s)-3,5-dimethylpiperazin-1-yl]benzamide |
| SCHEMBL63884 |
| SCHEMBL15250892 |
| rel-n-(5-(3,5-dimethoxyphenethyl)-1h-pyrazol-3-yl)-4-((3r,5s)-3,5-dimethylpiperazin-1-yl)benzamide |
| n-(5-(3,5-dimethoxyphenethyl)-1h-pyrazol-3-yl)-4-((3r,5s)-rel-3,5-dimethylpiperazin-1-yl)benzamide |
| n-(5-(3,5-dimethoxyphenethyl)-1h-pyrazol-3-yl)-4-((3r,5s)-3,5-dimethylpiperazin-1-yl)benzamide, rel- |
| AC-28442 |
| AKOS024464898 |
| DTXSID80145887 |
| mfcd22580423 |
| J-000994 |
| J-524217 |
| n-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1h-pyrazol-3-yl]-4-[(3s,5r)-3,5-dimethylpiperazin-1-yl]benzamide |
| NCGC00346713-05 |
| SW219341-1 |
| DB12247 |
| EX-A1578 |
| Q27074746 |
| AS-17054 |
| AMY16612 |
| CCG-269382 |
| nsc-799346 |
| nsc799346 |
| nsc-765338 |
| nsc765338 |
| nsc-764239 |
| nsc764239 |
| benzamide, n-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1h-pyrazol-3-yl]-4-[(3r,5s)-3,5-dimethyl-1-piperazinyl]-, rel- |
Research Excerpts
Overview
AZD4547 is a small molecule inhibitor of FGFR1. It has potent preclinical activity in FGFR2 amplified gastric adenocarcinoma SNU16 and SGC083 xenograft models.
Treatment
AZD4547 significantly alleviated the expression of the pro-inflammatory factors IL-1β, IL-6, TNF-α, MMP9, and CXCL10 both in vivo and in vitro. Treatment also significantly inhibited mRNA expression of inflammatory genes in the epidermis.
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| " Most common adverse events (AEs; any grade) were: dysgeusia (50% of patients); stomatitis (41%); diarrhoea (38%); hyperphosphataemia (38%); dry mouth (35%)." | ( Safety, tolerability and pharmacokinetics of the fibroblast growth factor receptor inhibitor AZD4547 in Japanese patients with advanced solid tumours: a Phase I study. Fujikawa, K; Fukao, T; Iwasa, S; Kitagawa, C; Kogure, Y; Landers, D; Sagawa, T; Saka, H; Takahashi, N; Takahashi, Y; Tchinou, C; Yamada, Y, 2017) | 0.67 |
| " The incidence of adverse events was similar in both treatment arms." | ( A randomized, open-label study of the efficacy and safety of AZD4547 monotherapy versus paclitaxel for the treatment of advanced gastric adenocarcinoma with FGFR2 polysomy or gene amplification. Bang, YJ; Chao, Y; Cunningham, D; Ferry, DR; Frewer, P; Kilgour, E; Landers, D; Mansoor, W; Petty, RD; Ratnayake, J; Smith, NR; Stockman, PK; Van Cutsem, E, 2017) | 0.7 |
Pharmacokinetics
| Excerpt | Reference | Relevance |
|---|---|---|
| "The challenge of developing effective pharmacodynamic biomarkers for preclinical and clinical testing of FGFR signaling inhibition is significant." | ( Identification of Pharmacodynamic Transcript Biomarkers in Response to FGFR Inhibition by AZD4547. Baker, D; Cross, S; Davies, BR; Delpuech, O; Dry, JR; Dymond, M; Kilgour, E; Mooney, L; Rooney, C; Shaw, R; Smith, PD; Veldman-Jones, M; Wang, D; Wilson, J; Zhang, P, 2016) | 0.66 |
| " Following single and multiple dosing, absorption rate appeared moderate; peak plasma concentrations generally occurred 3-4 h post-dose, then declined biphasically with terminal half-life ~30 h." | ( Safety, tolerability and pharmacokinetics of the fibroblast growth factor receptor inhibitor AZD4547 in Japanese patients with advanced solid tumours: a Phase I study. Fujikawa, K; Fukao, T; Iwasa, S; Kitagawa, C; Kogure, Y; Landers, D; Sagawa, T; Saka, H; Takahashi, N; Takahashi, Y; Tchinou, C; Yamada, Y, 2017) | 0.67 |
Compound-Compound Interactions
| Excerpt | Reference | Relevance |
|---|---|---|
| " The removal of AZD4547 from the optimized drug combination resulted in 80% of cell viability inhibition, while still maintaining the synergistic interaction." | ( A streamlined search technology for identification of synergistic drug combinations. Berndsen, RH; Ding, X; Dyson, PJ; Griffioen, AW; Ho, CM; Nowak-Sliwinska, P; van den Bergh, H; Weiss, A, 2015) | 0.76 |
| " To examine an alternative approach of integrin-based anti-osteosacoma strategy, acurhagin-C, a Glu-Cys-Asp (ECD)-disintegrin, was isolated and evaluated for its application in combination with two potent inhibitors of basic fibroblast growth factor (bFGF) and interleukin-8 (IL-8)." | ( Synergistic suppression of a disintegrin acurhagin-C in combination with AZD4547 and reparixin on terminating development for human osteosarcoma MG-63 cell. Chiang, TB; Shih, CH; Wang, WJ, 2017) | 0.69 |
| "We demonstrate a promising low-dose drug combination development to obtain drug combinations effective in naive as well as resistant tumours." | ( Identification of low-dose multidrug combinations for sunitinib-naive and pre-treated renal cell carcinoma. Achkhanian, J; Nowak-Sliwinska, P; Rausch, M; Rotari, A; Weiss, A, 2020) | 0.56 |
Bioavailability
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Roles (1)
| Role | Description |
|---|---|
| fibroblast growth factor receptor antagonist | An antagonist at the fibroblast growth factor receptor. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
Drug Classes (3)
| Class | Description |
|---|---|
| pyrazoles | |
| N-arylpiperazine | |
| benzamides | |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
Protein Targets (12)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Fumarate hydratase | Homo sapiens (human) | Potency | 37.2212 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| PPM1D protein | Homo sapiens (human) | Potency | 18.5569 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 16.2784 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
| polyprotein | Zika virus | Potency | 37.2212 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| Interferon beta | Homo sapiens (human) | Potency | 18.5569 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Aurora kinase A | Homo sapiens (human) | Kd | 0.3811 | 0.0001 | 0.7342 | 9.3000 | AID1342794 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (264)
Molecular Functions (31)
Ceullar Components (47)
Bioassays (178)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1516681 | Antiproliferative activity against human UMUC14 cells measured after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1193347 | Cytotoxicity against human HL7702 cells assessed as cell survival at 2 to 10 uM after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1313608 | Inhibition of recombinant human VEGFR2 using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1626475 | Inhibition of human FGFR2 using poly (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1626488 | Antitumor activity against human NCI-H1581 cells xenografted in nude mouse assessed as tumor growth inhibition at 12.5 mg/kg, po qd administered for 21 days | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1416442 | Inhibition of wild type non-phosphorylated N-terminal His6-tagged FGFR4 (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8 | Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
| AID1584406 | Antiproliferative activity against mouse BAF3 cells expressing TEL-fused KDR kinase after 72 hrs by CCK8 or MTT assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
| AID1176848 | Inhibition of FGFR2 (unknown origin) at 10 nM by ELISA method | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization. |
| AID1316518 | Antiproliferative activity against human RT112 cells after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20 | Synthesis of novel arylaminoquinazolinylurea derivatives and their antiproliferative activities against bladder cancer cell line. |
| AID1584401 | Antiproliferative activity against FGFR2 amplified human SNU16 cells after 72 hrs by CCK8 or MTT assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
| AID1717930 | Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1193339 | Inhibition of FGFR1 (unknown origin) after 90 mins by TR-FRET assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1298508 | Inhibition of recombinant FGFR2 in human SNU16 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 | Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1626474 | Volume of distribution in ICR mouse at 2 mg/kg, iv by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1484911 | Inhibition of FGFR1 (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3β inhibitors for the treatment of ovarian cancer. |
| AID1431267 | Inhibition of recombinant human FGFR4 in presence of ATP | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors. |
| AID1426086 | Antiproliferative activity against human SGC7901 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological evaluation, QSAR and molecular dynamics simulation studies of potential fibroblast growth factor receptor 1 inhibitors for the treatment of gastric cancer. |
| AID1193340 | Inhibition of FGFR2 (unknown origin) after 90 mins by TR-FRET assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1416443 | Inhibition of non-phosphorylated N-terminal His6-tagged FGFR4 C552A mutant (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8 | Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
| AID1613015 | Antiproliferative activity against FGFR2 amplified human SNU16 cells after 72 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. |
| AID1845304 | Inhibition of recombinant human FGFR4 in the presence of ATP at Km concentration | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
| AID1313644 | Antitumor activity against human NCI-H1581 cells xenografted in nude mouse assessed as tumor growth inhibition at 20 mg/kg administered as qd for 21 days measured on day 21 post last dose relative to vehicle-treated control | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1313641 | Antiproliferative activity against FGFR3-amplified human RT112 cells after 72 hrs by CCK8/MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1404606 | Antiproliferative activity against human SNU16 cells expressing FGFR2 after 72 hrs | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. |
| AID1298518 | Inhibition of recombinant FGFR4 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 | Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1313606 | Antiproliferative activity against FGFR1-amplified human NCI-H1581 cells after 72 hrs by CCK8/MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1717976 | Inhibition of wild-type FGFR4 (unknown origin) assessed as ratio of Kinact to Ki | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1626497 | Inhibition of human FGFR2 | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1626470 | Cmax in ICR mouse at 12.5 mg/kg administered as oral gavage by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1431265 | Inhibition of recombinant human FGFR2 in presence of ATP | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors. |
| AID1450773 | Inhibition of FGFR2 in human SNU16 cells assessed as inhibition of cell proliferation after 72 hrs by cell counting kit-8 assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1626491 | Protein binding in mouse plasma at 5 uM after 4 hrs by equilibrium dialysis assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1516684 | Antiproliferative activity against mouse BaF3/TEL-VEGFR2 cells measured after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1313605 | Inhibition of recombinant human FGFR1 using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1404604 | Antiproliferative activity against human KG1 cells expressing FGFR1 after 72 hrs | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. |
| AID1810715 | Antiproliferative activity against human SK-HEP1 cells expressing FGFR4 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery and Optimization of a Novel 2 |
| AID1431266 | Inhibition of recombinant human FGFR3 in presence of ATP | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors. |
| AID1613014 | Antiproliferative activity against FGFR1 fused human KG1 cells after 72 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. |
| AID1404607 | Antiproliferative activity against human RT112 cells expressing FGFR3 after 72 hrs | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. |
| AID1810713 | Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery and Optimization of a Novel 2 |
| AID1845305 | Inhibition of recombinant human KDR in the presence of ATP at Km concentration | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
| AID1298506 | Inhibition of recombinant FGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 | Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1416444 | Inhibition of non-phosphorylated N-terminal His6-tagged FGFR4 C477A mutant (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8 | Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
| AID1298524 | Inhibition of FGFR1 in human KG1 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 | Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1416438 | Inhibition of phosphorylated FGFR4 (388 to 802 residues) (unknown origin) using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8 | Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
| AID1298523 | Inhibition of FGFR1 in human H1581 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 | Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1626468 | AUC(0 to infinity) in ICR mouse at 2 mg/kg, iv by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1487617 | Antiproliferative activity against human KG1 cells after 72 hrs by CCK-8 assay | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16 | Optimization of 1H-indazol-3-amine derivatives as potent fibroblast growth factor receptor inhibitors. |
| AID1404609 | Antiproliferative activity against mouse BAF3 cells expressing VEGFR2 after 72 hrs | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. |
| AID1845302 | Inhibition of recombinant human FGFR2 in the presence of ATP at Km concentration | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
| AID1516666 | Inhibition of human VEGFR2 using poly (Glu, Tyr)4:1 as substrate measured after 60 mins by ELISA | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1584423 | Inhibition of FGFR4 (unknown origin) | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
| AID1717908 | Hepatic extraction ratio in rat liver microsomes preincubated for 3 mins followed by NADPH addition and measured after 60 mins | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1516661 | Inhibition of human FGFR1 using poly (Glu, Tyr)4:1 as substrate measured after 60 mins by ELISA | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1450763 | Inhibition of FGFR1OP2 fused FGFR1 in human KG1 cells assessed as inhibition of cell proliferation after 72 hrs by cell counting kit-8 assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1810704 | Inhibition of human FGFR3 (450 to 758 residues) expressed in Escherichia coli BL21 (DE3) by HTRF assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery and Optimization of a Novel 2 |
| AID1613038 | Inhibition of FGFR2 phosphorylation in human SNU-16 cells at 50 nM after 2 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. |
| AID1584402 | Antiproliferative activity against FGFR3 amplified human OPM2 cells after 72 hrs by CCK8 or MTT assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
| AID1626462 | Inhibition of recombinant human FGFR1 using poly (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1717910 | Inhibition of FGFR4 in mouse BAF3 cells assessed as reduction in cell viability incubated for 2 days by cell proliferation assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1626500 | Inhibition of human VEGFR2 | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1516665 | Inhibition of human FGFR4 using poly (Glu, Tyr)4:1 as substrate measured after 60 mins by ELISA | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1487616 | Antiproliferative activity against human SNU16 cells after 72 hrs by CCK-8 assay | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16 | Optimization of 1H-indazol-3-amine derivatives as potent fibroblast growth factor receptor inhibitors. |
| AID1717977 | Inhibition of wild-type FGFR4 C477A mutant (unknown origin) assessed as ratio of Kinact to Ki | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1584379 | Antiproliferative activity against FGFR1 amplified human NCI-H1581 cells after 72 hrs by CCK8 or MTT assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
| AID1450766 | Inhibition of FGFR3 in human RT112 cells assessed as inhibition of cell proliferation after 72 hrs by cell counting kit-8 assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1810714 | Antiproliferative activity against human SNU-16 cells expressing FGFR2 assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery and Optimization of a Novel 2 |
| AID1626487 | Antiproliferative activity against human RT112 cells after 72 hrs by CCK-8 assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1404608 | Antiproliferative activity against human UM-UC-14 cells expressing FGFR3 after 72 hrs | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. |
| AID1450764 | Inhibition of FGFR2 in human KATO III cells assessed as inhibition of cell proliferation after 72 hrs by cell counting kit-8 assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1626484 | Antiproliferative activity against human KG1 cells after 72 hrs by CCK-8 assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1435470 | Antitumor activity against FGFR1-amplified human NCI-H1581 cells xenografted in nude mouse assessed as tumor growth inhibition at 20 mg/kg, po qd administered for 10 days and measured on day 10 post last dose relative to vehicle-treated control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. |
| AID1626467 | Half life in ICR mouse at 12.5 mg/kg administered as oral gavage by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1516663 | Inhibition of human FGFR2 using poly (Glu, Tyr)4:1 as substrate measured after 60 mins by ELISA | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1626476 | Inhibition of human FGFR3 using poly (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1810702 | Inhibition of human FGFR1 (459 to 765 residues) expressed in Escherichia coli BL21 (DE3) by HTRF assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery and Optimization of a Novel 2 |
| AID1193342 | Inhibition of FGFR4 (unknown origin) after 90 mins by TR-FRET assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1516683 | Antiproliferative activity against mouse BaF3/TEL-FGFR1 cells measured after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1193343 | Cytotoxicity against human A549 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1626471 | AUC(0 to infinity) in ICR mouse at 12.5 mg/kg administered as oral gavage by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1313640 | Antiproliferative activity against FGFR2-amplified human SNU16 cells after 72 hrs by CCK8/MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1487618 | Inhibition of recombinant FGFR2 (unknown origin) using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA based spectrophotometric analysis | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16 | Optimization of 1H-indazol-3-amine derivatives as potent fibroblast growth factor receptor inhibitors. |
| AID1313639 | Antiproliferative activity against FGFR1-translocated human KG1 cells after 72 hrs by CCK8/MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1450705 | Inhibition of recombinant human FGFR3 using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1626464 | Antiproliferative activity against human NCI-H1581 cells after 72 hrs by CCK-8 assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1404603 | Inhibition of recombinant FGFR1 (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA based spectrophotometric method | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. |
| AID1450703 | Inhibition of recombinant human FGFR1 using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1626472 | Clearance in ICR mouse at 2 mg/kg, iv by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1613017 | Antiproliferative activity against human UM-UC-14 cells harboring FGFR3 mutation after 72 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. |
| AID1450735 | Inhibition of FGFR1 in human NCI-H1581 cells assessed as inhibition of cell proliferation after 72 hrs by cell counting kit-8 assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1404605 | Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 after 72 hrs | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors. |
| AID1626498 | Inhibition of human FGFR3 | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1845303 | Inhibition of recombinant human FGFR3 in the presence of ATP at Km concentration | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
| AID1626485 | Antiproliferative activity against human SNU16 cells after 72 hrs by CCK-8 assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1298525 | Inhibition of FGFR2 in human KATO III cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 | Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1516662 | Antiproliferative activity against human KG1 cells measured after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1584377 | Inhibition of recombinant FGFR1 (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
| AID1313647 | Inhibition of recombinant human FGFR4 | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1626477 | Inhibition of human FGFR4 using poly (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1298517 | Inhibition of recombinant FGFR3 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 | Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1450704 | Inhibition of recombinant human FGFR2 using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1176847 | Inhibition of FGFR1 (unknown origin) at 10 nM by ELISA method | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization. |
| AID1298515 | Selectivity ratio of IC50 for recombinant VEGFR2 (unknown origin) to IC50 for recombinant FGFR2 (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 | Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1810716 | Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery and Optimization of a Novel 2 |
| AID1516695 | Irreversible inhibition of human FGFR1 using poly (Glu, Tyr)4:1 as substrate measured after 60 mins by caliper assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1416440 | Inhibition of phosphorylated FGFR2 (406 to 821 residues) (unknown origin) using 5-Fluo-Ahx-EEPLYWSFPAKKKCONH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8 | Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
| AID1845301 | Inhibition of recombinant human FGFR1 in the presence of ATP at Km concentration | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
| AID1626466 | Half life in ICR mouse at 2 mg/kg, iv by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1810717 | Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth measured after 96 hrs by CCK-8 assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery and Optimization of a Novel 2 |
| AID1426088 | Antiproliferative activity against human BGC823 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological evaluation, QSAR and molecular dynamics simulation studies of potential fibroblast growth factor receptor 1 inhibitors for the treatment of gastric cancer. |
| AID1298516 | Inhibition of recombinant FGFR1 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 | Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1584404 | Antiproliferative activity against FGF19/FGFR4 expressing human HuH7 cells after 72 hrs by CCK8 or MTT assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
| AID1778528 | Inhibition of recombinant human FGFR1 in presence of ATP at Km concentration | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors. |
| AID1626463 | Inhibition of recombinant human VEGFR2 using poly (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1416439 | Inhibition of phosphorylated FGFR1 (407 to 822 residues) (unknown origin) using 5-Fluo-Ahx-EEPLYWSFPAKKKCONH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8 | Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
| AID1810705 | Inhibition of human FGFR4 (445 to 753 residues) expressed in Escherichia coli BL21 (DE3) by HTRF assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery and Optimization of a Novel 2 |
| AID1845250 | Antiproliferative activity against human SNU-16 cells overexpressing FGFR2 assessed as inhibition of cell proliferative by measuring ATP level after 72 hrs by luminescence based assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). |
| AID1626473 | Oral bioavailability in ICR mouse at 12.5 mg/kg administered as gavage by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1313609 | Selectivity ratio of IC50 for recombinant human VEGFR2 to IC50 for recombinant human FGFR1 | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. |
| AID1516664 | Inhibition of human FGFR3 using poly (Glu, Tyr)4:1 as substrate measured after 60 mins by ELISA | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1778530 | Inhibition of recombinant human FGFR3 in presence of ATP at Km concentration | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors. |
| AID1416441 | Inhibition of phosphorylated FGFR3 (411 to 806 residues) (unknown origin) using 5-Fluo-Ahx-EEPLYWSFPAKKKCONH2 as substrate after 60 mins by microfluidic mobility shift assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8 | Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region. |
| AID1193341 | Inhibition of FGFR3 (unknown origin) after 90 mins by TR-FRET assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1487619 | Inhibition of recombinant FGFR1 (unknown origin) using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA based spectrophotometric analysis | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16 | Optimization of 1H-indazol-3-amine derivatives as potent fibroblast growth factor receptor inhibitors. |
| AID1516682 | Antiproliferative activity against human SNU16 cells measured after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16 | Discovery and Development of a Series of Pyrazolo[3,4- |
| AID1193344 | Cytotoxicity against human HeLa 229 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1626496 | Inhibition of human FGFR1 | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1298526 | Inhibition of FGFR3 in human RT112 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 | Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1584405 | Antiproliferative activity against mouse BAF3 cells expressing TEL-fused FGFR4 kinase after 72 hrs by CCK8 or MTT assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
| AID1193345 | Cytotoxicity against mouse B16F10 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1626486 | Antiproliferative activity against human KATO III cells after 72 hrs by CCK-8 assay | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1584403 | Antiproliferative activity against FGFR3 amplified human RT112 cells after 72 hrs by CCK8 or MTT assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors. |
| AID1426087 | Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological evaluation, QSAR and molecular dynamics simulation studies of potential fibroblast growth factor receptor 1 inhibitors for the treatment of gastric cancer. |
| AID1193346 | Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1431264 | Inhibition of recombinant human FGFR1 in presence of ATP | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors. |
| AID1612907 | Inhibition of FGFR1 (unknown origin) after 60 mins by ELISA | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. |
| AID1298514 | Inhibition of recombinant VEGFR2 (unknown origin) using (Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 | Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors. |
| AID1613016 | Antiproliferative activity against FGFR2 amplified human NCI-H716 cells after 72 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. |
| AID1810703 | Inhibition of human FGFR2 (458 to 768 residues) expressed in Escherichia coli BL21 (DE3) by HTRF assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Discovery and Optimization of a Novel 2 |
| AID1626499 | Inhibition of human FGFR4 | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1717911 | Inhibition of FGFR4 in mouse BAF3 cells assessed as decrease in FGFR4 phosphorylation incubated for 40 mins | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. |
| AID1778529 | Inhibition of recombinant human FGFR2 in presence of ATP at Km concentration | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors. |
| AID1626469 | Cmax in ICR mouse at 2 mg/kg, iv by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Jun-09, Volume: 7, Issue:6 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. |
| AID1450765 | Inhibition of FGFR3 mutant in human UM-UC-14 cells assessed as inhibition of cell proliferation after 72 hrs by cell counting kit-8 assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1345514 | Human fibroblast growth factor receptor 1 (Type V RTKs: FGF (fibroblast growth factor) receptor family) | 2015 | Organic & biomolecular chemistry, Jul-28, Volume: 13, Issue:28 | Design, synthesis and biological evaluation of novel FGFR inhibitors bearing an indazole scaffold. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (117)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 84 (71.79) | 24.3611 |
| 2020's | 33 (28.21) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 35.17
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.
| This Compound (35.17) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 6 (5.13%) | 5.53% |
| Reviews | 3 (2.56%) | 6.00% |
| Case Studies | 1 (0.85%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 107 (91.45%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||