Assay ID | Title | Year | Journal | Article |
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. |
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. |
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. |
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. |
AID717051 | Permeability across apical to basolateral side in human Caco2 cells | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. |
AID634556 | Selectivity for human CHK1 over human BRSK1 | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634546 | Antimitotic activity in etoposide-induced human HT-29 cells assessed as induction of M-phase phosphoprotein 2 expression by ELISA | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634548 | Inhibition of human CHK1 at 1 uM | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634555 | Selectivity for human CHK1 over human RSK1 | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634558 | Selectivity for human CHK1 over human BRSK2 | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634565 | Efflux ratio of permeability across apical to basolateral side over basolateral to apical side in human Caco2 cells | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID719553 | Inhibition of human ERG overexpressed in HEK cells | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. |
AID634569 | Antitumor activity against human SW620 cells xenografted in nude SCID mouse assessed as delay in tumor growth at 25 to 50 mg/kg, ip | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634549 | Inhibition of human RSK1 at 1 uM | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID719556 | Ratio of GI50 for human HT-29 cells to IC50 for CHK1-mediated abrogation of etoposide-induced G2 check point arrest in human HT-29 cells | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. |
AID634563 | Drug metabolism in human liver microsomes after 30 mins | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID719559 | Inhibition of CHK1 using 5-FAM-KKKVSRSGLYRSPSMPENLNRPR-COOH as substrate after 1 hr by microfluidic assay in presence of ATP | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. |
AID634562 | Drug metabolism in mouse liver microsomes after 30 mins | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634564 | Effective permeability across apical to basolateral side in human Caco2 cells | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634545 | Cytotoxicity against human HT-29 cells after 96 hrs by SRB assay | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID719554 | Potentiation index, ratio of IC50 for human SW620 cells to IC50 for potentiation of gemcitabine-induced cytotoxicity in human SW620 cells | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. |
AID719582 | Oral bioavailability in BALB/c mouse at 10 mg/kg | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. |
AID634553 | Inhibition of human RSK2 at 1 uM | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634559 | Selectivity for human CHK1 over human RSK2 | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID717052 | Drug metabolism in mouse liver microsomes after 30 mins | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. |
AID634554 | Inhibition of human NUAK1 at 1 uM | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634551 | Inhibition of human IRAK1 at 1 uM | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634561 | Drug metabolism in rat liver microsomes after 30 mins | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID719546 | Inhibition of CHK1 in human SW620 cells assessed as potentiation of gemcitabine-induced cytotoxicity after 24 to 48 hrs | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. |
AID634543 | Competitive inhibition of human CHK2 using ATP as substrate by DELFIA | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634557 | Selectivity for human CHK1 over human IRAK1 | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634547 | Potentiation of SN38-induced cytotoxicity in human HT-29 cells after 96 hrs by SRB assay relative to control | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634568 | Potentiation of irinotecan-induced antitumor activity against human SW620 cells xenografted in nude SCID mouse assessed as delay in tumor growth at 40 mg/kg, ip | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID719557 | Inhibition of CHK1 in human HT-29 cells assessed as etoposide-induced G2 check point arrest after 21 hrs by ELISA | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. |
AID634550 | Inhibition of human BRSK1 at 1 uM | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634567 | In vivo inhibition of irinotecan-induced CHK1 phosphorylation at Ser296 residue in human SW620 cells xenografted in nude SCID mouse at 40 mg/kg, ip after 24 hrs by Western blot analysis | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634566 | Oral bioavailability in SCID mouse at 40 mg/kg | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID634560 | Selectivity for human CHK1 over human NUAK1 | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID719550 | Inhibition of CDK1 | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. |
AID634552 | Inhibition of human BRSK2 at 1 uM | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
AID719555 | Potentiation index, ratio of IC50 for human HT-29 cells to IC50 for potentiation of gemcitabine-induced cytotoxicity in human HT-29 cells | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. |
AID634542 | Competitive inhibition of human CHK1 using ATP as substrate by DELFIA | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. |
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. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |