| Assay ID | Title | Year | Journal | Article |
|---|
| AID1198687 | Growth inhibition of human SKBR3 cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1201541 | Inhibition of TRKB (unknown origin) | 2015 | European journal of medicinal chemistry, 05-05, Volume: 95 | Drug discovery using spirooxindole cores: Success and Challenges [corrected]. |
| AID1201544 | Inhibition of PLK-3 (unknown origin) | 2015 | European journal of medicinal chemistry, 05-05, Volume: 95 | Drug discovery using spirooxindole cores: Success and Challenges [corrected]. |
| AID1198665 | Inhibition of CYP1A2 (unknown origin) by fluorescence assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198678 | Half life in Sprague-Dawley rat at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198721 | Antitumor activity against human HCT116 cells xenografted in athymic CD-1 nude mouse assessed as tumor growth inhibition at MTD, po qd administered 1-on/3-off schedule up to day 21 | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198679 | AUC(infinity) in Sprague-Dawley rat at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198667 | Inhibition of CYP2C9 (unknown origin) by fluorescence assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198666 | Inhibition of CYP2D6 (unknown origin) by fluorescence assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1870309 | Cytotoxicity against human NCI-H596 cells assessed as reduction in cell viability measured after 6 days by MTT assay | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B. |
| AID1198691 | Growth inhibition of human OVCAR3 cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198706 | Inhibition of TIE2 (unknown origin) by cell-based assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1201537 | Inhibition of FGFR1 (unknown origin) | 2015 | European journal of medicinal chemistry, 05-05, Volume: 95 | Drug discovery using spirooxindole cores: Success and Challenges [corrected]. |
| AID1201539 | Inhibition of TIE2/TEK (unknown origin) | 2015 | European journal of medicinal chemistry, 05-05, Volume: 95 | Drug discovery using spirooxindole cores: Success and Challenges [corrected]. |
| AID1201536 | Inhibition of AURKB (unknown origin) | 2015 | European journal of medicinal chemistry, 05-05, Volume: 95 | Drug discovery using spirooxindole cores: Success and Challenges [corrected]. |
| AID1198717 | Antitumor activity against human A549 cells xenografted in CB-17 SCID mouse assessed as tumor growth inhibition at 3 mg/kg, po qd administered for 21 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198663 | Growth inhibition of human MDA-MB-231 cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198714 | Antitumor activity against human MDA-MB-468 cells xenografted in CB-17 SCID mouse assessed as tumor growth inhibition at 9.4 mg/kg, po qd administered for 21 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1870307 | Cytotoxicity against human NCI-H23 cells assessed as reduction in cell viability measured after 6 days by MTT assay | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B. |
| AID1201543 | Inhibition of PLK-2 (unknown origin) | 2015 | European journal of medicinal chemistry, 05-05, Volume: 95 | Drug discovery using spirooxindole cores: Success and Challenges [corrected]. |
| AID1198703 | Inhibition of PLK4 (unknown origin) by cell-based assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198707 | Inhibition of TRKA (unknown origin) by cell-based assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198675 | Cmax in athymic CD1 nude mouse at 25 mg/kg, po by LC/MS/MS analysis | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198710 | Selectivity ratio of EC50 for AURKB/INCENP (unknown origin) to EC50 for PLK4 (unknown origin) by cell-based assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1870313 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 6 days by MTT assay | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B. |
| AID1198692 | Growth inhibition of human SW620 cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198684 | AUC(infinity) in beagle dog at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198683 | Half life in beagle dog at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198694 | Growth inhibition of human HCT116 cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1870315 | Cytotoxicity against human DU-145 cells assessed as reduction in cell viability measured after 6 days by MTT assay | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B. |
| AID1198671 | Half life in mouse liver microsomes | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1201534 | Inhibition of PLK-4 (unknown origin) | 2015 | European journal of medicinal chemistry, 05-05, Volume: 95 | Drug discovery using spirooxindole cores: Success and Challenges [corrected]. |
| AID1201542 | Inhibition of PLK-1 (unknown origin) | 2015 | European journal of medicinal chemistry, 05-05, Volume: 95 | Drug discovery using spirooxindole cores: Success and Challenges [corrected]. |
| AID1198696 | Inhibition of PLK2 (unknown origin) at 50 uM by FRET analysis | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198722 | Antitumor activity against human HCT116 cells xenografted in athymic CD-1 nude mouse assessed as tumor growth inhibition at MTD, po qd administered 1-on/3-off schedule up to day 21 measured on day 35 | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198662 | Growth inhibition of human HCC1954 cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198713 | Antitumor activity against human MDA-MB-468 cells xenografted in CB-17 SCID mouse assessed as tumor growth inhibition at 3 mg/kg, po qd administered for 21 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1201540 | Inhibition of TRKA (unknown origin) | 2015 | European journal of medicinal chemistry, 05-05, Volume: 95 | Drug discovery using spirooxindole cores: Success and Challenges [corrected]. |
| AID1870308 | Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability measured after 6 days by MTT assay | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B. |
| AID1198688 | Growth inhibition of human CAL51 cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198709 | Competitive binding to PLK4 (unknown origin) by double reciprocal plot analysis in presence of ATP | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198677 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198686 | Oral bioavailability in beagle dog at 5 mg/kg | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198711 | Toxicity in CB-17 SCID mouse xenografted with human MDA-MB-468 cells assessed as mortality at 3 to 9.4 mg/kg, po qd administered for 21 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198690 | Growth inhibition of human A549 cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198715 | Antitumor activity against human SW620 cells xenografted in CB-17 SCID mouse assessed as tumor growth inhibition at 3 mg/kg, po qd administered for 21 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198695 | Inhibition of PLK1 (unknown origin) at 50 uM by FRET analysis | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198689 | Growth inhibition of human BT20 cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198716 | Antitumor activity against human SW620 cells xenografted in CB-17 SCID mouse assessed as tumor growth inhibition at 9.4 mg/kg, po qd administered for 21 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198674 | Half life in human liver microsomes | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198704 | Inhibition of AURKA (unknown origin) by cell-based assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198697 | Inhibition of PLK3 (unknown origin) at 50 uM by FRET analysis | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1870316 | Inhibition of AURKB (unknown origin) | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B. |
| AID1870314 | Cytotoxicity against human NCI-N87 cells assessed as reduction in cell viability measured after 6 days by MTT assay | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B. |
| AID1198670 | Inhibition of CYP3A4 (unknown origin) using BFC as substrate by fluorescence assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198720 | Toxicity in po dosed athymic CD-1 nude mouse xenografted with human HCT116 cells administered qd 1-on/3-off schedule up to day 21 | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1860515 | Inhibition of PLK4 (unknown origin) by Lanthascreen Eu Kinase binding assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer. |
| AID1201545 | Competitive inhibition of PLK-4 (unknown origin) | 2015 | European journal of medicinal chemistry, 05-05, Volume: 95 | Drug discovery using spirooxindole cores: Success and Challenges [corrected]. |
| AID1201538 | Inhibition of SLC34A2/ROS (unknown origin) | 2015 | European journal of medicinal chemistry, 05-05, Volume: 95 | Drug discovery using spirooxindole cores: Success and Challenges [corrected]. |
| AID1198681 | Oral bioavailability in Sprague-Dawley rat at 5 mg/kg | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198659 | Inhibition of PLK4 (unknown origin) by ELISA | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198669 | Inhibition of CYP3A4 (unknown origin) using DBF as substrate by fluorescence assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198668 | Inhibition of CYP2C19 (unknown origin) by fluorescence assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1870311 | Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 6 days by MTT assay | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B. |
| AID1198680 | AUC(infinity) in Sprague-Dawley rat at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198682 | Clearance in beagle dog at 1 mg/kg, iv | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1870310 | Cytotoxicity against human Calu-6 cells assessed as reduction in cell viability measured after 6 days by MTT assay | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B. |
| AID1198708 | Inhibition of TRKB (unknown origin) by cell-based assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198701 | Inhibition of TRKA (unknown origin) by FRET analysis | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198676 | AUC in athymic CD1 nude mouse at 25 mg/kg, po by LC/MS/MS analysis | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1201535 | Inhibition of AURKA (unknown origin) | 2015 | European journal of medicinal chemistry, 05-05, Volume: 95 | Drug discovery using spirooxindole cores: Success and Challenges [corrected]. |
| AID1198660 | Growth inhibition of human MDA-MB-468 cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198661 | Growth inhibition of human MCF7 cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198705 | Inhibition of AURKB/INCENP (unknown origin) by cell-based assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198718 | Antitumor activity against human A549 cells xenografted in CB-17 SCID mouse assessed as tumor growth inhibition at 9.4 mg/kg, po qd administered for 21 days | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198693 | Growth inhibition of human COLO205 cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198712 | Toxicity in CB-17 SCID mouse xenografted with human MDA-MB-468 cells assessed as loss in body weight at 3 to 9.4 mg/kg, po qd administered for 21 days relative to control | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198672 | Half life in rat liver microsomes | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198700 | Inhibition of TIE2 (unknown origin) by FRET analysis | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198673 | Half life in dog liver microsomes | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198698 | Inhibition of AURKA (unknown origin) by FRET analysis | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1870312 | Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 6 days by MTT assay | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B. |
| AID1198664 | Growth inhibition of human HMEC cells after 5 days by SRB assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198685 | AUC(infinity) in beagle dog at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198699 | Inhibition of AURKB/INCENP (unknown origin) by FRET analysis | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| AID1198702 | Inhibition of TRKB (unknown origin) by FRET analysis | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor ag |
| 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] |