Assay ID | Title | Year | Journal | Article |
AID617779 | Inhibition of PAK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617415 | Cytotoxicity against human SKOV3 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID1375009 | Inhibition of recombinant human CDK9/cyclin T1 using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate after 90 mins by fluorescence assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
| Discovery of novel CDK inhibitors via scaffold hopping from CAN508. |
AID272433 | Activity of PKBalpha at 10 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID272418 | Inhibition of CDK2/Cyclin E in presence of 100 uM ATP | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617724 | Inhibition of MLK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617627 | Inhibition of HIPK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617390 | Cytotoxicity against human NCI-H23 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617295 | Cytotoxicity against human SF295 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617626 | Inhibition of HER4 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617704 | Inhibition of IKK-epsilon assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617618 | Inhibition of EPH-B3 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616322 | Antiangiogenic activity against HUVEC cells assessed as inhibition of VEGF-induced cell migration-associated wound closure at >10 uM after 16 hrs by microscopic analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272441 | Cell cycle arrest in HT29 cells by accumulation at G0/G1 phase at 50 uM after 12 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID1194736 | Cytotoxicity against human K562 cells after 72 hrs by calcein AM staining-based fluorescence assay | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
| Novel arylazopyrazole inhibitors of cyclin-dependent kinases. |
AID617776 | Inhibition of p38beta MAPK assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617398 | Cytotoxicity against human RPMI8226 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617705 | Inhibition of IR assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617777 | Inhibition of p38delta MAPK assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID1194738 | Cytotoxicity against human RPMI8226 cells after 72 hrs by calcein AM staining-based fluorescence assay | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
| Novel arylazopyrazole inhibitors of cyclin-dependent kinases. |
AID616301 | Inhibition of PKCzeta assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616303 | Inhibition of PLK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617611 | Inhibition of CDK9/cyclin T assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272417 | Inhibition of CDK2/Cyclin E | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID272443 | Cell cycle arrest in HT29 cells by accumulation at G2/M phase at 50 uM after 12 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617785 | Inhibition of PIM1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272467 | Inhibition of EpCAM mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 3 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617773 | Inhibition of NEK6 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617400 | Cytotoxicity against human LOXIMVI cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617707 | Inhibition of IRR assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617782 | Inhibition of PAK6 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617725 | Inhibition of MLK3 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617516 | Inhibition of CDK9-catalyzed RNA polymerase 2 phosphorylation at Ser2 in human HMEC1 cells after 2 hrs by immunoblotting | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617714 | Inhibition of MAPKAP-K2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617720 | Inhibition of MEKK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272423 | Inhibition of CDK9/Cyclin T1 in presence of 100 uM ATP | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID616302 | Inhibition of PKD1 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617519 | Inhibition of CDK9 by [33P]gamma-ATP incorporation assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617391 | Cytotoxicity against human NCI-H322M cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272422 | Inhibition of CDK7/Cyclin H in presence of 100 uM ATP | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID272434 | Activity of SAPK2-alpha at 10 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID272416 | Viability of K562 cells at 100 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617771 | Inhibition of MST4 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616311 | Inhibition of SGK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272419 | Inhibition of CDK1/Cyclin B in presence of 100 uM ATP | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617790 | Inhibition of PKBbeta assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID723732 | Stabilization of CDK2/Cyclin A (174 to 432 amino acid residues) (unknown origin) assessed as change in melting temperature at 20 uM by differential scanning fluorimetry assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity. |
AID723735 | Inhibition of CDK9/Cyclin T (1 to 330 amino acid residues) (unknown origin) by differential scanning fluorimetry assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity. |
AID617423 | Cytotoxicity against human SN12C cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272410 | Antiproliferative activity against HOS cell line | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617394 | Cytotoxicity against human CCRF-CEM cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272424 | Activity of CDK9/Cyclin T1 at 10 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID1689408 | Inhibition of human full-length N-terminal GST/His6-tagged CDK9 (1 to 372 residues)/His6-tagged Cyclin-T1 (1 to 726 residues) expressed in sf9 cells using (YSPTSPS)2KK peptide as substrate in presence of [gamma33P]ATP | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. |
AID617706 | Inhibition of IRAK4 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617769 | Inhibition of MSK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272469 | Inhibition of EpCAM mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 12 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617422 | Cytotoxicity against human RXF393 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617620 | Inhibition of ERK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616319 | Inhibition of TTK assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617612 | Inhibition of CK1delta assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617506 | Antiangiogenic activity in VEGF-stimulated HMEC1 assessed as reduction in median length of tube at 20 uM after 16 hrs by photographic analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617719 | Inhibition of MARK4 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272466 | Inhibition of EpCAM mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617723 | Inhibition of MKK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617625 | Inhibition of GSK3b assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617709 | Inhibition of JNK1A1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617393 | Cytotoxicity against human NCI-H522 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617526 | Inhibition of CAMK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617503 | Antiangiogenic activity against HUVEC cells assessed as inhibition of VEGF-induced cell migration-associated wound closure after 16 hrs by microscopic analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617502 | Antiproliferative activity against HMEC1 cells assessed as decrease in cell viability at >50 uM within 72 hrs by calcein AM staining-based fluorescence assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616310 | Inhibition of S6K1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617300 | Cytotoxicity against human COLO205 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617408 | Cytotoxicity against human UACC62 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617419 | Cytotoxicity against human A498 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617781 | Inhibition of PAK5 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616321 | Inhibition of YES1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617291 | Cytotoxicity against human MCF7 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617722 | Inhibition of MINK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272454 | Decrease in pRb phosphorylation in MCF7 cells after 24 hrs at 50 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617716 | Inhibition of MARK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617768 | Inhibition of MNK2alpha assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617619 | Inhibition of EPH-B4 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617298 | Cytotoxicity against human SNB75 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617616 | Inhibition of EPHA2 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617524 | Inhibition of BRSK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617518 | Inhibition of CDK7-catalyzed RNA polymerase 2 phosphorylation at Ser5 in human HMEC1 cells at 5 to 40 uM after 2 hrs by immunoblotting | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617416 | Cytotoxicity against human DU145 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617418 | Cytotoxicity against human 786-0 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616315 | Inhibition of SYK assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272482 | Increase in p53 expression level in MCF7 cells at 100 uM after 24 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID272421 | Inhibition of CDK4/Cyclin D1 in presence of 100 uM ATP | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617629 | Inhibition of HIPK3 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617622 | Inhibition of ERK8 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272455 | Increase in p53 expression level in MCF7 cells at 50 uM after 24 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID616304 | Inhibition of PRAK assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617783 | Inhibition of PDK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617523 | Inhibition of BRSK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617420 | Cytotoxicity against human ACHN cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617302 | Cytotoxicity against human HCT116 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617407 | Cytotoxicity against human UACC257 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617304 | Cytotoxicity against human HT-29 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272457 | Reduction of RNA polymerase 2 CTD phosphorylation in MCF7 cells after 24 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617632 | Inhibition of IGF-1R assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617509 | Decrease in VEGF expression in human MCF7 cells at >10 uM after 24 hrs by sandwich ELISA | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617289 | Cytotoxicity against human BT549 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617402 | Cytotoxicity against human MALME-3M cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272460 | Inhibition of GAPDH mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 6 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617787 | Inhibition of PIM3 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272425 | Activity of CDK2/Cyclin E at 10 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617613 | Inhibition of CK2alpha assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272432 | Activity of PKA at 10 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617521 | Inhibition of Aurora A assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617708 | Inhibition of JAK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617789 | Inhibition of PKBalpha assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617305 | Cytotoxicity against human KM12 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616307 | Inhibition of ROCK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617772 | Inhibition of NEK2a assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617296 | Cytotoxicity against human SF539 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID1194741 | Inhibition of CDK7/cyclin H (unknown origin) expressed in baculovirus infected Sf9 cells | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
| Novel arylazopyrazole inhibitors of cyclin-dependent kinases. |
AID617401 | Cytotoxicity against human M14 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617711 | Inhibition of JNK2alpha2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617412 | Cytotoxicity against human OVCAR4 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617780 | Inhibition of PAK4 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272465 | Inhibition of CEA mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 12 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617778 | Inhibition of p38-gamma MAPK assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617395 | Cytotoxicity against human HL-60(TB) cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617299 | Cytotoxicity against human U251 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617309 | Cytotoxicity against human HOP62 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272420 | Inhibition of CDK2/Cyclin A in presence of 100 uM ATP | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID616308 | Inhibition of RSK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617411 | Cytotoxicity against human OVCAR3 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617770 | Inhibition of MST2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID723734 | Inhibition of CDK2/Cyclin A (174 to 432 amino acid residues) (unknown origin) by differential scanning fluorimetry assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity. |
AID272431 | Activity of P70S6K at 10 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID1194737 | Cytotoxicity against human MCF7 cells after 72 hrs by calcein AM staining-based fluorescence assay | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
| Novel arylazopyrazole inhibitors of cyclin-dependent kinases. |
AID617775 | Inhibition of p38alpha MAPK assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272408 | Inhibition of CDK2/Cyclin E in presence of 15 uM ATP | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617426 | Antiproliferative activity against HUVEC cells assessed as decrease in cell viability at >50 uM within 72 hrs by calcein AM staining-based fluorescence assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617712 | Inhibition of JNK3alpha1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617425 | Cytotoxicity against human UO31 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617292 | Cytotoxicity against human MDA-MB-231 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617786 | Inhibition of PIM2 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617520 | Inhibition of AMPK assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272430 | Activity of MAPK1 at 10 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID616410 | Antiproliferative activity against HUVEC cells assessed as decrease in cell viability at 10 to 40 uM within 72 hrs by calcein AM staining-based fluorescence assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272412 | Antiproliferative activity against K562 cell line | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617710 | Inhibition of Lck assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272440 | Cell cycle arrest in HT29 cells by accumulation at G2/M phase at 50 uM after 6 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID1375008 | Inhibition of recombinant human CDK2/cyclin A using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate after 15 mins by fluorescence assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
| Discovery of novel CDK inhibitors via scaffold hopping from CAN508. |
AID617294 | Cytotoxicity against human SF268 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617307 | Cytotoxicity against human A549 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616312 | Inhibition of SmMLCK assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272439 | Cell cycle arrest in HT29 cells by accumulation at S phase at 50 uM after 6 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617389 | Cytotoxicity against human NCI-H226 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617788 | Inhibition of PKA assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616306 | Inhibition of RIPK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272461 | Inhibition of GAPDH mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 12 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617512 | Inhibition of TNF-alpha-induced Nuclear factor-kappa-B-mediated ICAM-1 expression in human HMEC1 cells after 24 hrs by FACS analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617392 | Cytotoxicity against human NCI-H460 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617409 | Cytotoxicity against human IGROV1 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617414 | Cytotoxicity against human OVCAR8 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617623 | Inhibition of FGF-R1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617522 | Inhibition of Aurora B assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617721 | Inhibition of MELK assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617791 | Inhibition of PKCalpha assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617507 | Antiangiogenic activity in VEGF-stimulated HMEC1 assessed as reduction in median length of tube at 40 uM after 16 hrs by photographic analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617410 | Cytotoxicity against human NCI/ADR-RES cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272483 | Inhibition of P70S6K | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617397 | Cytotoxicity against human MOLT4 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617624 | Inhibition of GCK assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272409 | Antiproliferative activity against MCF7 cell line | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617306 | Cytotoxicity against human SW620 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272438 | Cell cycle arrest in HT29 cells by accumulation at G0/G1 phase at 50 uM after 6 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617784 | Inhibition of PHKG1 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616411 | Antiproliferative activity against HMEC1 cells assessed as decrease in cell viability at 10 to 40 uM within 72 hrs by calcein AM staining-based fluorescence assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616313 | Inhibition of Src assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617774 | Inhibition of NUAK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617718 | Inhibition of MARK3 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617767 | Inhibition of MNK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617405 | Cytotoxicity against human SK-MEL-28 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617628 | Inhibition of HIPK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617717 | Inhibition of MARK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272436 | Cell cycle arrest in HT29 cells by accumulation at S phase at 50 uM after 3 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID1689407 | Inhibition of CDK2/cyclin E (unknown origin) expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate in presence of [gamma33P]ATP | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. |
AID616314 | Inhibition of SRPK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616318 | Inhibition of TrkA assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617630 | Inhibition of CHK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617609 | Inhibition of CAMKKbeta assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617417 | Cytotoxicity against human PC3 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617310 | Cytotoxicity against human HOP92 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617293 | Cytotoxicity against human T47D cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272468 | Inhibition of EpCAM mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 6 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID272463 | Inhibition of CEA mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 3 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID272411 | Antiproliferative activity against G361 cell line | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617413 | Cytotoxicity against human OVCAR5 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617515 | Inhibition of CDK9-catalyzed RNA polymerase 2 phosphorylation at Ser2 in human MCF7 cells after 2 hrs by immunoblotting | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272427 | Activity of CHK1 at 10 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID272456 | Increase in p21 WAF1 expression level in MCF7 cells at 50 uM after 24 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID272453 | Decrease in pRb phosphorylation in MCF7 cells after 24 hrs at 25 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID1194742 | Inhibition of CDK9/cyclin T1 (unknown origin) expressed in baculovirus infected Sf9 cells | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
| Novel arylazopyrazole inhibitors of cyclin-dependent kinases. |
AID272413 | Viability of MCF7 cells at 100 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617505 | Antiangiogenic activity in VEGF-stimulated HMEC1 assessed as reduction in total length of tube at 40 uM after 16 hrs by photographic analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617631 | Inhibition of CHK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617610 | Inhibition of CDK2/cyclin A assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617396 | Cytotoxicity against human K562 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617514 | Inhibition of RNA synthesis in human HMEC1 cells assessed as decrease in [3H] Uridine incorporation after 2 hrs by scintillation counting | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617614 | Inhibition of CSK assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617715 | Inhibition of MAPKAP-K3 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616320 | Inhibition of VEGFR assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272459 | Inhibition of GAPDH mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 3 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617399 | Cytotoxicity against human SR cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617308 | Cytotoxicity against human EKVX cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617617 | Inhibition of EPHA4 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617517 | Inhibition of CDK7-catalyzed RNA polymerase 2 phosphorylation at Ser5 in human MCF7 cells at 5 to 40 uM after 2 hrs by immunoblotting | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617421 | Cytotoxicity against human Caki1 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272415 | Viability of G361 cells at 100 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617504 | Antiangiogenic activity in VEGF-stimulated HMEC1 assessed as reduction in total length of tube at 20 uM after 16 hrs by photographic analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616316 | Inhibition of TAK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617621 | Inhibition of ERK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616309 | Inhibition of RSK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617297 | Cytotoxicity against human SNB19 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617303 | Cytotoxicity against human HCT15 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617424 | Cytotoxicity against human TK10 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID1194739 | Inhibition of CDK1/cyclin B (unknown origin) expressed in baculovirus infected Sf9 cells | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
| Novel arylazopyrazole inhibitors of cyclin-dependent kinases. |
AID617703 | Inhibition of IKK-beta assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617301 | Cytotoxicity against human HCC2998 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID1194740 | Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected Sf9 cells | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
| Novel arylazopyrazole inhibitors of cyclin-dependent kinases. |
AID617403 | Cytotoxicity against human MDA-MB-435 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272428 | Activity of CK2 at 10 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617511 | Decrease in VEGF expression in human DU145 cells at >10 uM after 24 hrs by sandwich ELISA | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617404 | Cytotoxicity against human SK-MEL-2 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616317 | Inhibition of TBK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617525 | Inhibition of BTK assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617615 | Inhibition of EF2K assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272464 | Inhibition of CEA mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 6 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617513 | Inhibition of RNA synthesis in human MCF7 cells assessed as decrease in [3H] Uridine incorporation after 2 hrs by scintillation counting | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID1194735 | Inhibition of CDK2/cyclin E (unknown origin) expressed in baculovirus infected Sf9 cells | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
| Novel arylazopyrazole inhibitors of cyclin-dependent kinases. |
AID617406 | Cytotoxicity against human SK-MEL-5 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID617508 | Antiangiogenic activity in VEGF-stimulated HMEC1 assessed as reduction in tube nodes after 16 hrs by photographic analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272462 | Inhibition of CEA mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617290 | Cytotoxicity against human Hs 578T cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID616305 | Inhibition of PRK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID723733 | Stabilization of CDK9/Cyclin T (1 to 330 amino acid residues) (unknown origin) assessed as change in melting temperature at 20 uM by differential scanning fluorimetry assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity. |
AID617510 | Decrease in VEGF expression in human MDA-MB-231 cells at >10 uM after 24 hrs by sandwich ELISA | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272458 | Inhibition of GAPDH mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID272426 | Activity of c-ABL at 10 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID272414 | Viability of HOS cells at 100 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID272442 | Cell cycle arrest in HT29 cells by accumulation at S phase at 50 uM after 12 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID617713 | Inhibition of LKB1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
AID272429 | Activity of GSK3-beta at 10 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID272435 | Cell cycle arrest in HT29 cells by accumulation at G0/G1 phase at 50 uM after 3 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID272437 | Cell cycle arrest in HT29 cells by accumulation at G2/M phase at 50 uM after 3 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID1800495 | Kinase Selectivity from Article 10.1111/cbdd.12330: \\Arylazopyrazole AAP1742 inhibits CDKs and induces apoptosis in multiple myeloma cells via Mcl-1 downregulation.\\ | 2014 | Chemical biology & drug design, Oct, Volume: 84, Issue:4
| Arylazopyrazole AAP1742 inhibits CDKs and induces apoptosis in multiple myeloma cells via Mcl-1 downregulation. |
AID1796840 | CDK Inhibition Assay from Article 10.1021/jm0605740: \\4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.\\ | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
| 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| The selective P-TEFb inhibitor CAN508 targets angiogenesis. |
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. |
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. |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2012 | ACS chemical biology, May-18, Volume: 7, Issue:5
| The CDK9 C-helix exhibits conformational plasticity that may explain the selectivity of CAN508. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |