Assay ID | Title | Year | Journal | Article |
AID1731804 | Growth inhibition human KG-1a cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1295778 | Inhibition of WNT pathway activation in human COLO205 cells expressing APC mutant | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1731798 | Inhibition of human GSKalpha S449A mutant (2 to 3nd residues) using YRRAAVPPSPSLSRHSSPHQS(p) EDEEE as substrate incubated for 40 mins in presence of [gamma-33P]-ATP by scintillation counting method | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1198348 | Antitumor activity against human COLO205-F1756 clone 4 cells harboring APC mutant xenografted in CrTac:NCr-Foxn1nu mouse assessed as reduction in flux normalized to tumor weight at 70 mg/kg, po bid for 9 days relative to control | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1198311 | Tmax in NMRI mouse at 0.2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731820 | Growth inhibition human WI38 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731868 | Toxicity in BALB/c mouse assessed as monocytes at 70 mg/kg, po administered once daily for 7 days and measured on day 15 by flow cytometric analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1295752 | Clearance in NMRI mouse at 0.2 mg/kg, iv and 0.5 mg/kg po by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1852094 | Antiproliferative activity against human HT-29 cells assessed as cell viability incubated for 48 hrs by MTT assay | | | |
AID1198329 | Inhibition of CYP2C9 (unknown origin) | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1198328 | Thermodynamic aqueous solubility of the compound in phosphate buffer at pH 7.4 | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731866 | Toxicity in BALB/c mouse assessed as dendritic cells at 70 mg/kg, po administered once daily for 7 days and measured on day 15 by flow cytometric analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1198314 | Tmax in NMRI mouse at 0.5 mg/kg, po | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1198347 | Antitumor activity against human COLO205-F1756 clone 4 cells harboring APC mutant xenografted in CrTac:NCr-Foxn1nu mouse assessed as reduction in tumor weight at 70 mg/kg, po bid for 9 days relative to control | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731805 | Growth inhibition human MOLM-13 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1295775 | Inhibition of WNT pathway activation in human LS174T cells expressing beta-catenin mutant | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1852096 | Antiproliferative activity against human CT26 cells assessed as cell viability incubated for 48 hrs by MTT assay | | | |
AID1731812 | Growth inhibition human COLO 205 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1198308 | Intrinsic clearance in human liver microsome at 1 uM preincubated for 5 mins by LC-MS analysis | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1295754 | Volume of distribution in NMRI mouse assessed as liver blood flow at 0.2 mg/kg, iv and 0.5 mg/kg, po by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1852095 | Antiproliferative activity against human SW480 cells assessed as cell viability incubated for 48 hrs by MTT assay | | | |
AID1852092 | Inhibition of CDK8 (unknown origin) assessed as inhibition rate | | | |
AID1198349 | Drug uptake in tumor of human COLO205-F1756 clone 4 cells harboring APC mutant xenografted CrTac:NCr-Foxn1nu mouse at 70 mg/kg, po bid for 9 days measured after 2 to 6 hrs | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1295761 | Clearance in Beagle dog at 0.2 mg/kg, iv and 0.5 mg/kg, po by LC-MS/MS analysis relative to liver blood flow | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1198342 | Inhibition of ligand-induced WNT3A signaling in human PA-1 cells harboring TCF preincubated for 6 hrs before ligand addition measured after 24 hrs by luciferase reporter assay | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731815 | Growth inhibition human PANC-1 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1198338 | Inhibition of WNT signaling in human 7dF3 cells assessed as inhibition of endogenous cMYC transcription up to 9.1 uM after 2 hrs by RT-PCR analysis relative to control | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731865 | Toxicity in BALB/c mouse assessed as B cells at 70 mg/kg, po administered once daily for 7 days and measured on day 15 by flow cytometric analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1198331 | Inhibition of CYP2C8 (unknown origin) | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1198345 | Effect on TCF1 level in human COLO205-F1756 clone 4 cells harboring APC mutant and TCF/LEF responsive element at 350 nM by immunoblotting | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1295770 | Thermodynamic solubility of compound | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1198317 | Clearance in Wistar rat at 0.2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1295781 | Half life in NMRI mouse at 0.2 mg/kg, iv and 0.5 mg/kg, po by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1295764 | Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assay | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1198306 | Intrinsic clearance in mouse liver microsome at 1 uM preincubated for 5 mins by LC-MS analysis | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1295766 | Intrinsic clearance in rat microsomes preincubated for 5 mins followed by addition of 1.5 mM of NADPH measured after 5 to 30 mins by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1198336 | Inhibition of GSK3alpha (unknown origin) | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1198321 | Half life in Wistar rat at 0.2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1198335 | Efflux ratio for apparent permeability in human Caco2 cells after 2 hrs by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731802 | Growth inhibition human Kasumi-1 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731803 | Growth inhibition human KG-1 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731859 | Toxicity in BALB/c mouse assessed as vasculitis in blood vessels at 70 mg/kg, po administered once daily for 7 days and measured on day 15 | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1295777 | Inhibition of WNT pathway activation in human SW480 cells expressing APC mutant | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1731814 | Growth inhibition human HT-29 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1198323 | AUC in Wistar rat at 0.5 mg/kg, po | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731838 | Cmax in Sprague-Dawley rat at 20 mg/kg, po measured up to 24 hrs by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1198312 | AUC in NMRI mouse at 0.2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1295769 | Kinetic solubility of compound | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1731811 | Growth inhibition human U-937 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1852097 | Cytotoxicity against human GES1 cells assessed as cell viability incubated for 48 hrs by MTT assay | | | |
AID1198340 | Inhibition of basal WNT signaling in human LS174T cells harboring beta-catenin mutant and TCF/LEF responsive element after 24 hrs by firefly luciferase reporter assay | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1198341 | Inhibition of basal WNT signaling in human SW480 cells harboring APC mutant | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1198316 | Oral bioavailability in NMRI mouse at 0.5 mg/kg | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1198350 | Drug uptake in plasma of human COLO205-F1756 clone 4 cells harboring APC mutant xenografted CrTac:NCr-Foxn1nu mouse at 70 mg/kg, po bid for 9 days measured after 2 to 6 hrs | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1198320 | AUC in Wistar rat at 0.2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731864 | Toxicity in BALB/c mouse assessed as increase in dead splenocytes at 70 mg/kg, po administered once daily for 7 days and measured on day 15 by flow cytometric analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1295749 | Binding affinity to CDK8/CDK19 in human 7dF3 cells preincubated for 2 hrs followed by addition 10 uM of beta-oestradiol measured after 24 hrs by luciferase reporter gene assay | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1731819 | Growth inhibition human MDA-MB-453 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1198343 | Inhibition of WNT signaling in human RKO-F1522 cells after 24 hrs by EF1alpha promoter-driven luciferase reporter assay | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1198324 | Oral bioavailability in Wistar rat at 0.5 mg/kg | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731834 | Half life in Sprague-Dawley rat at 5 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1295771 | Plasma clearance in wild type mouse | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1731818 | Growth inhibition human MDA-MB-231 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731809 | Growth inhibition human PL-21 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731840 | Half life in Sprague-Dawley rat at 20 mg/kg, po measured up to 24 hrs by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1295759 | Clearance in Wistar rat at 0.2 mg/kg, iv and 0.5 mg/kg po by LC-MS/MS analysis relative to liver blood flow | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1731862 | Toxicity in BALB/c mouse assessed as pathological alterations in left femora at 70 mg/kg, po administered once daily for 7 days and measured on day 15 | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1295750 | Efflux ratio in human Caco2 cells after 2 hrs by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1295756 | Clearance in Beagle dog at 0.2 mg/kg, iv and 0.5 mg/kg, po by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1295782 | Half life in Wistar rat at 0.2 mg/kg, iv and 0.5 mg/kg po by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1295760 | Volume of distribution in Wistar rat assessed as liver blood flow at 0.2 mg/kg, iv and 0.5 mg/kg po by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1731799 | Inhibition of human GSKbeta H350L mutant (2 to 3nd residues) using YRRAAVPPSPSLSRHSSPHQS(p) EDEEE as substrate incubated for 40 mins in presence of [gamma-33P]-ATP by scintillation counting method | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731867 | Toxicity in BALB/c mouse assessed as granulocytes at 70 mg/kg, po administered once daily for 7 days and measured on day 15 by flow cytometric analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1198307 | Intrinsic clearance in rat liver microsome at 1 uM preincubated for 5 mins by LC-MS analysis | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731832 | Cmax in Sprague-Dawley rat at 5 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731872 | Growth inhibition human T47D cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731817 | Growth inhibition human MCF7 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731777 | Growth inhibition of human MV4-11 cells after 72 hrs by resazurin staining based assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1295765 | Binding affinity to human CDK19 (1 to 502 amino acid residues)/Cyclin C (1 to 283 amino acid residues) by reporter displacement assay | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1198346 | Effect on TCF4 level in human COLO205-F1756 clone 4 cells harboring APC mutant and TCF/LEF responsive element at 350 nM by immunoblotting | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1295757 | Oral bioavailability NMRI mouse assessed as liver blood flow at 0.5 mg/kg by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1731863 | Toxicity in BALB/c mouse assessed as pathological alterations in lung at 70 mg/kg, po administered once daily for 7 days and measured on day 15 | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1295776 | Inhibition of WNT ligand dependent WNT pathway activation in human PA1 cells | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1198313 | Half life in NMRI mouse at 0.2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1295768 | Intrinsic clearance in human microsomes preincubated for 5 mins followed by addition of 1.5 mM of NADPH measured after 5 to 30 mins by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1731860 | Toxicity in BALB/c mouse assessed as infiltration of inflammatory cells at 70 mg/kg, po administered once daily for 7 days and measured on day 15 | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731871 | Toxicity in BALB/c mouse assessed as increase in CD3-T cells at 70 mg/kg, po administered once daily for 7 days and measured on day 15 by flow cytometric analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1198309 | Clearance in NMRI mouse at 0.2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731813 | Growth inhibition human HCT-116 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1295755 | Oral bioavailability in Wistar rat at 0.5 mg/kg by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1295772 | Drug excretion in wild type mouse feces assessed as parent compound remaining level | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1295762 | Volume of distribution in Beagle dog at 0.2 mg/kg, iv and 0.5 mg/kg, po by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1198332 | Inhibition of CYP3A4 (unknown origin) | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731837 | Clearance in Sprague-Dawley rat at 5 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1198327 | Kinetic solubility of the compound in phosphate buffer at pH 7.4 | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731870 | Toxicity in BALB/c mouse assessed as neutrophils at 70 mg/kg, po administered once daily for 7 days and measured on day 15 by flow cytometric analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731816 | Growth inhibition human A2780 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731869 | Toxicity in BALB/c mouse assessed as macrophages at 70 mg/kg, po administered once daily for 7 days and measured on day 15 by flow cytometric analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731833 | Tmax in Sprague-Dawley rat at 5 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1198318 | Volume of distribution at steady state in Wistar rat at 0.2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1198325 | Inhibition of GST-tagged TNKS1 (1023 to 1327 aa) (unknown origin) after 90 mins by HTRF assay | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731857 | Toxicity in BALB/c mouse assessed as interstitial pneumonitis in lung at 70 mg/kg, po administered once daily for 7 days and measured on day 15 | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731836 | Volume of distribution at steady state in Sprague-Dawley rat at 5 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1198344 | Inhibition of basal WNT signaling in human COLO205-F1756 clone 4 cells harboring APC mutant and TCF/LEF responsive element after 24 hrs by firefly luciferase reporter assay | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731835 | AUC in Sprague-Dawley rat at 5 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1295767 | Intrinsic clearance in mouse microsomes preincubated for 5 mins followed by addition of 1.5 mM of NADPH measured after 5 to 30 mins by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1731841 | AUC in Sprague-Dawley rat at 20 mg/kg, po measured up to 24 hrs by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731858 | Toxicity in BALB/c mouse assessed as increase in number of alveolar macrophages at 70 mg/kg, po administered once daily for 7 days and measured on day 15 | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1295784 | Lipophilicity, logD of the compound | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1295783 | Half life in Beagle dog at 0.2 mg/kg, iv and 0.5 mg/kg, po by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1852091 | Inhibition of CDK8 (unknown origin) assessed as inhibition rate at 200 nM relative to control | | | |
AID1731842 | Oral bioavailability in Sprague-Dawley rat at 20 mg/kg measured up to 24 hrs by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1198315 | AUC in NMRI mouse at 0.5 mg/kg, po | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731800 | Inhibition of human full length PKCtheta using histone H1 as substrate incubated for 40 mins in presence of [gamma-33P]-ATP by scintillation counting method | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731808 | Inhibition of CDK8 in human MV4-11 cells assessed as reduction in STAT1 phosphorylation at s727 residues at 1 to 5 times of GI50 concentration after 2 hrs by Western blot analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731861 | Toxicity in BALB/c mouse assessed as destruction of vessel walls at 70 mg/kg, po administered once daily for 7 days and measured on day 15 | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1295758 | Clearance in Wistar rat at 0.2 mg/kg, iv and 0.5 mg/kg po by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1198326 | Inhibition of GST-tagged TNKS2 (873 to 1166 aa) (unknown origin) after 90 mins by HTRF assay | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1295773 | Plasma clearance in P-gp KO mouse | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1198296 | Inhibition of WNT signaling in human 7dF3 cells preincubated for 2 hrs before beta-estradiol addition measured after 24 hrs by luciferase reporter assay | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731839 | Tmax in Sprague-Dawley rat at 20 mg/kg, po measured up to 24 hrs by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731807 | Effect on total STAT1 level in human MV4-11 cells at 1 to 5 times of GI50 concentration after 2 hrs by Western blot analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1295774 | Drug excretion in P-gp knock-out mouse feces assessed as parent compound remaining level | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1198339 | Inhibition of WNT signaling in human 7dF3 cells assessed as inhibition of endogenous cMYC transcription after 2 hrs by RT-PCR analysis | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1852093 | Antiproliferative activity against human HCT-116 cells assessed as cell viability incubated for 48 hrs by MTT assay | | | |
AID1295763 | Oral bioavailability in Beagle dog at 0.5 mg/kg by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1731806 | Growth inhibition human NB4 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1198322 | Tmax in Wistar rat at 0.5 mg/kg, po | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731810 | Growth inhibition human THP1 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1198337 | Inhibition of GSK3beta (unknown origin) | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1295753 | Clearance in NMRI mouse at 0.2 mg/kg, iv and 0.5 mg/kg, po by LC-MS/MS analysis relative to liver blood flow | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. |
AID1198319 | Tmax in Wistar rat at 0.2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1198310 | Volume of distribution at steady state in NMRI mouse at 0.2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
| Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. |
AID1731776 | Inhibition of CDK8/cyclin C (unknown origin) using RBER-IRStide as substrate incubated for 60 mins in presence of [gamma33P]ATP by scintillation counting method | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
AID1731801 | Growth inhibition human HL-60 cells after 72 hrs by resazurin or MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. |
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. |
AID1347414 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence | 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. |
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. |
AID1345673 | Human cyclin dependent kinase 19 (CDK8 subfamily) | 2015 | Nature chemical biology, Dec, Volume: 11, Issue:12
| A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. |
AID1345661 | Human cyclin dependent kinase 8 (CDK8 subfamily) | 2015 | Nature chemical biology, Dec, Volume: 11, Issue:12
| A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |