| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| AID164187 | Displacement of [3H]- PDBu from Protein kinase C theta C1b domain | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
| Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V. |
| AID163180 | Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C alpha C1b domain | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID163847 | Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C epsilon C1b domain | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID501104 | Induction of human HUES8 differentiation into pancreatic lineage assessed as increase in somatostatin-producing endocrine cells at 300 nM after 4 days by immunostaining | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID163673 | Ratio of binding to PKC delta C1b domain wild type and mutant (Thr12 to Gly) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID321016 | Displacement of [3H]PDBu from PKCtheta C1B domain | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
| Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction. |
| AID501134 | Induction of ISL1 expression in CD1 nude mouse heart at 300 nM after 4 days by fluorescent confocal microscopy | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501113 | Induction of mouse AV3 cell differentiation into pancreatic lineage assessed as increase in Nkx2.2 mRNA expression at 300 nM after 6 days by RT-PCR analysis pretreated with 1000 ng/ml recombinant mouse Nodal for 5 days | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501103 | Induction of human HUES8 differentiation into pancreatic lineage assessed as increase in DBA-positive exocrine cells at 300 nM after 4 days by RT-PCR (Rvb (DMSO) = 0%) | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID163370 | Displacement of [3H]- PDBu from Protein kinase C beta C1b domain | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
| Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V. |
| AID321011 | Displacement of [3H]PDBu from PKCgamma C1A domain | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
| Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction. |
| AID501128 | Induction of FABP2 expression in CD1 nude mouse intestine at 300 nM after 4 days by fluorescent confocal microscopy | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501096 | Effect on glucagon expression in human HUES8 insulin-producing cells at 300 nM after 4 days by immunocytochemistry (Rvb = 75.2 +/- 9.1%) | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501130 | Induction of Albumin expression in CD1 nude mouse liver at 300 nM after 4 days by fluorescent confocal microscopy | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501120 | Inhibition of PKC signaling in human HUES8 cells assessed as decrease in Pdx1-expressing cells at 4 uM after 4 days by immunocytochemistry in presence of ILV pregrown in medium with Wnt3a, activin A, FGF10, KAAD-cyclopamine and retinoic acid (Rvb = 26.9+/ | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501098 | Effect on human HUES8 differentiation into neuronal lineage assessed as c-peptide/GFAP double positive cells at 300 nM after 4 days by immunocytochemistry | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID163545 | Binding of Indolactam-V(ILV) to mutant Protein kinase C delta C1b domain (Leu24 to Gly) (Not determined) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID501136 | Induction of MYOD expression in CD1 nude mouse mesoderm at 300 nM after 4 days by fluorescent confocal microscopy | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID1870485 | Inhibition of GLI in SAG induced mouse Sufu-KO-LIGHT cells assessed as residual Smo-independent Gli luciferase activity in starvation medium at 100 nM incubated for 30 hrs by dual luciferase assay | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Indolactam Dipeptides as Nanomolar Gli Inhibitors. |
| AID164182 | Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C theta C1a domain (Not tested) | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID501090 | Induction of human HUES8 cell differentiation into pancreatic progenitor cell assessed as increase in NGN3 mRNA expression at 300 nM after 4 days by RT-PCR analysis cells pregrown in medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic aci | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501076 | Induction of human HUES8 cell differentiation into pancreatic progenitor cells assessed as increase in Pdx1-expression in cells pregrown with medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic acid at 300 nM after 4 days by Opera high co | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID1870480 | Inhibition of GLI in SAG induced mouse Shh Light II cells assessed as residual Smo-dependent Gli luciferase activity in starvation medium incubated for 30 hrs by dual luciferase assay | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Indolactam Dipeptides as Nanomolar Gli Inhibitors. |
| AID501086 | Induction of human HUES8 cell differentiation into pancreatic progenitor cell assessed as increase in SOX9 mRNA expression at 300 nM after 4 days by RT-PCR analysis cells pregrown in medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic aci | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501106 | Induction of mouse AV3 Pdx1-expressing cell differentiation assessed as increase in SOX9 expression at 300 nM after 6 days by immunohistochemistry pretreated with 1000 ng/ml recombinant mouse Nodal for 5 days | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501107 | Induction of mouse AV3 Pdx1-expressing cell differentiation assessed as increase in Nkx6.1 expression at 300 nM after 6 days by immunohistochemistry pretreated with 1000 ng/ml recombinant mouse Nodal for 5 days | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501119 | Inhibition of PKC signaling in human HUES8 cells assessed as decrease in Pdx1-expressing cells at 1 uM after 4 days cells pregrown in medium with Wnt3a, activin A, FGF10, KAAD-cyclopamine and retinoic acid in presence of 10 uM Go 6983 by immunocytochemist | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID164183 | Displacement of [3H]- PDBu from Protein kinase C theta C1a domain (Not tested) | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
| Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V. |
| AID312190 | Displacement of [3H]PDBu from PKCtheta C1B domain | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID163365 | Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C beta C1a | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID163181 | Displacement of [3H]- PDBu from Protein kinase C alpha C1b domain | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
| Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V. |
| AID155888 | Displacement of [3H]PDBu from protein kinase C delta C1b domain (Wild type) | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID501081 | Induction of human HUES8 cell differentiation into pancreatic progenitor cell assessed as NKX6.1 expression in cells pregrown in medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic acid at 300 nM after 4 days by immunocytochemistry relati | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID163528 | Displacement of [3H]PDBu from recombinant Protein kinase C delta | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Clarification of the binding mode of teleocidin and benzolactams to the Cys2 domain of protein kinase Cdelta by synthesis of hydrophobically modified, teleocidin-mimicking benzolactams and computational docking simulation. |
| AID80959 | Tested for epstein barr virus early antigen (EBV-EA) inducing activity in differentiated HL-60 cells at 10e-7 M | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID163874 | Displacement of [3H]- PDBu from Protein kinase C eta C1b domain | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
| Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V. |
| AID312192 | Displacement of [3H]PDBu from PKCgamma C1A P11dfP mutant | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID1870487 | Inhibition of GLI in mouse ASZ001 cells assessed as reduction in cell viability in starvation medium at 1.5 uM incubated for 48 hrs by CellTiter assay relative to control | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Indolactam Dipeptides as Nanomolar Gli Inhibitors. |
| AID155891 | Displacement of [3H]PDBu from protein kinase C delta C1b domain mutant (L24G) (Not determined) | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID232112 | Ratio of binding affinity to PKC delta C1b domain wild type versus mutant P11G | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID164047 | Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C eta C1a domain | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID163669 | Ratio of binding to PKC delta C1b domain wild type and mutant (Gln27 to Val) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID321008 | Displacement of [3H]PDBu from PKCbeta C1B domain | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
| Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction. |
| AID501075 | Cytotoxicity against human HUES9 cells at 300 nM | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID1870484 | Inhibition of GLI in SAG induced mouse Sufu-KO-LIGHT cells assessed as residual Smo-independent Gli luciferase activity in starvation medium incubated for 30 hrs by dual luciferase assay | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Indolactam Dipeptides as Nanomolar Gli Inhibitors. |
| AID312189 | Displacement of [3H]PDBu from PKCeta C1B domain | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID501084 | Induction of human HUES8 cell differentiation into pancreatic progenitor cell assessed as increase in HNF6 mRNA expression at 300 nM after 4 days by RT-PCR analysis cells pregrown in medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic aci | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501089 | Induction of human HUES8 cell differentiation into endocrine progenitor cell assessed as increase in NKX2.2 mRNA expression at 300 nM after 4 days by RT-PCR analysis cells pregrown in medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic ac | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID321012 | Displacement of [3H]PDBu from PKCgamma C1B domain | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
| Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction. |
| AID501087 | Induction of human HUES8 cell differentiation into pancreatic progenitor cell assessed as increase in HB9 mRNA expression at 300 nM after 4 days by RT-PCR analysis pregrown in medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic acid | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID163666 | Binding of Indolactam-V(ILV) to mutant Protein kinase C delta C1b domain (Trp22 to Gly) (Not determined) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID155893 | Displacement of [3H]PDBu from protein kinase C delta C1b domain mutant (Q27Q) (Not determined) | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID163366 | Displacement of [3H]- PDBu from Protein kinase C beta C1a domain | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
| Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V. |
| AID80957 | Tested for epstein barr virus early antigen (EBV-EA) inducing activity in differentiated HL-60 cells at 10e-5 M | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID232117 | Ratio of binding affinity to PKC delta C1b domain wild type versus mutant T8G | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID163843 | Displacement of [3H]- PDBu from Protein kinase C epsilon C1a domain | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
| Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V. |
| AID501074 | Induction of human HUES9 cell differentiation into pancreatic lineage assessed as increase in Pdx1-expression in cells pregrown with medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic acid after 1 day by Opera high content screening syst | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID1870482 | Inhibition of GLI in SAG induced mouse C3H10T1/2 cells assessed reduction Gli-dependent differentiation by measuring ALP activity incubated for 48 hrs by chemiluminescence assay | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Indolactam Dipeptides as Nanomolar Gli Inhibitors. |
| AID232109 | Ratio of binding affinity to PKC delta C1b domain wild type versus mutant L20G | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID163872 | Displacement of [3H]- PDBu from Protein kinase C eta C1a domain | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
| Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V. |
| AID80961 | Tested for superoxide (O2-) generation inducing activity in differentiated HL-60 cells at 10e-5 M | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID501110 | Induction of mouse AV3 cell differentiation into pancreatic lineage assessed as increase in ptf1a mRNA expression at 300 nM after 6 days by RT-PCR analysis pretreated with 1000 ng/ml recombinant mouse Nodal for 5 days | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501115 | Induction of human HUES8 differentiation into definitive endoderm assessed as expression of SOX17 at 300 nM after 3 days by immunocytochemistry in presence of Wnt3a and activin A | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID155883 | Displacement of [3H]-PDBu from protein kinase C delta C1b domain mutant (P11G) | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID155886 | Displacement of [3H]PDBu from protein kinase C delta C1b domain mutant (T8G) | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID501083 | Induction of human HUES8 cell differentiation into pancreatic progenitor cell assessed as increase in Pdx1 mRNA expression at 300 nM after 4 days by RT-PCR analysis cells pregrown in medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic aci | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID163371 | Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C beta C1b domain | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID501082 | Induction of human HUES8 cell differentiation into pancreatic progenitor cell assessed as PTF1A expression in cells pregrown in medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic acid at 300 nM after 4 days by immunocytochemistry relativ | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID312191 | Displacement of [3H]PDBu from PKCdelta C1B P11dfP mutant | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID1870481 | Inhibition of GLI in SAG induced mouse Shh Light II cells assessed as residual Smo-dependent Gli luciferase activity in starvation medium at 100 nM incubated for 30 hrs by dual luciferase assay | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Indolactam Dipeptides as Nanomolar Gli Inhibitors. |
| AID312185 | Displacement of [3H]PDBu from PKCgamma C1A domain | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID501131 | Induction of BARX1 expression in CD1 nude mouse stomach at 300 nM after 4 days by fluorescent confocal microscopy | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID312200 | Induction of GFP-tagged PKC-beta-1 translocation in HeLa cells assessed as ratio of protein level in plasma membrane to cytosol at 1 uM | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID501079 | Induction of human HUES8 cell differentiation into pancreatic progenitor cell assessed as FOXA2 expression in cells pregrown in medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic acid at 300 nM after 4 days by immunocytochemistry relativ | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID232115 | Ratio of binding affinity to PKC delta C1b domain wild type versus mutant Q27V | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID501100 | Induction of human HUES8 differentiation into pancreatic lineage assessed as increase in amylase/CPA double-positive exocrine cells at 300 nM after 4 days by RT-PCR (Rvb = 1.6+/-0.2%) | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID321013 | Displacement of [3H]PDBu from PKCdelta C1B domain | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
| Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction. |
| AID163848 | Displacement of [3H]- PDBu from Protein kinase C epsilon C1b domain | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
| Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V. |
| AID164167 | Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C eta C1b domain | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID163193 | Displacement of [3H]- PDBu from recombinant PKC beta expressed in baculovirus | 1997 | Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
| Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivit |
| AID321015 | Displacement of [3H]PDBu from PKCeta C1B domain | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
| Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction. |
| AID501291 | Induction of insulin production in differentiated human HUES8 cells at 300 nM after 4 days by immunocytochemistry (Rvb = 0.2+/-0.1%) | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501097 | Effect on human HUES8 differentiation into neuronal lineage assessed as c-peptide/betaIIItubulin double positive cells at 300 nM after 4 days by immunocytochemistry | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID163842 | Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C epsilon C1a domain | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID501095 | Induction of Pdx1 expression in human HUES8 insulin-producing cells at 300 nM after 4 days by immunocytochemistry relative to control | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID80963 | Tested for superoxide (O2-) generation inducing activity in differentiated HL-60 cells at 10e-7 M | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID501073 | Induction of human HUES9 cell differentiation into pancreatic lineage assessed as increase in Pdx1-expression in cells pregrown with medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic acid at 1 uM after 1 day by Opera high content screen | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID164037 | Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C gamma C1b domain | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID163526 | Displacement of [3H]- PDBu from recombinant PKC delta expressed in baculovirus | 1997 | Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
| Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivit |
| AID166231 | Binding affinity against RAS guanyl releasing protein using [3H]- PDBu as the labeled ligand | 2002 | Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
| Structural basis of RasGRP binding to high-affinity PKC ligands. |
| AID501133 | Induction of Troponin T expression in CD1 nude mouse heart at 300 nM after 4 days by fluorescent confocal microscopy | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID312187 | Displacement of [3H]PDBu from PKCdelta C1B domain | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID163674 | Ratio of binding to PKC delta C1b domain wild type and mutant (Tyr8 to Gly) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID155884 | Displacement of [3H]PDBu from protein kinase C delta C1b domain mutant (Q27V) | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID501088 | Induction of human HUES8 cell differentiation into pancreatic progenitor cell assessed as increase in PROX1 mRNA expression at 300 nM after 4 days by RT-PCR analysis cells pregrown in medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic ac | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501118 | Inhibition of PKC signaling in human HUES8 cells assessed as decrease in Pdx1-expressing cells at 1 uM after 4 days cells pregrown in medium with Wnt3a, activin A, FGF10, KAAD-cyclopamine and retinoic acid in presence of 1 uM BISI by immunocytochemistry ( | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501101 | Induction of human HUES8 differentiation into pancreatic lineage assessed as increase in amylase/CPA double-positive exocrine cells at 300 nM after 4 days by RT-PCR (Rvb (DMSO) = 0.2+/-0.1%) | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501125 | Induction of SOX7 expression in CD1 nude mouse extra-embryonic endoderm at 300 nM after 4 days by fluorescent confocal microscopy | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID312181 | Displacement of [3H]PDBu from PKCalpha C1A domain | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID163664 | Binding of Indolactam-V(ILV) to mutant Protein kinase C delta C1b domain (Thr12 to Gly) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID312182 | Displacement of [3H]PDBu from PKCalpha C1B domain | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID163537 | Binding of Indolactam-V(ILV) to mutant Protein kinase C delta C1b domain (Gln27 to Gly) (Not determined) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID312188 | Displacement of [3H]PDBu from PKCepsilon C1B domain | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID81280 | Effective concentration against monocytes of HL-60 cells growth inhibition | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| Clarification of the binding mode of teleocidin and benzolactams to the Cys2 domain of protein kinase Cdelta by synthesis of hydrophobically modified, teleocidin-mimicking benzolactams and computational docking simulation. |
| AID155885 | Displacement of [3H]PDBu from protein kinase C delta C1b domain mutant (T12G) | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID164025 | Displacement of [3H]- PDBu from recombinant PKC gamma expressed in baculovirus | 1997 | Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
| Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivit |
| AID312194 | Selectivity ratio of PKCgamma C1A domain over PKCgamma C1A P11dfP mutant | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID163667 | Binding of Indolactam-V(ILV) to mutant Protein kinase C delta C1b domain (Tyr8 to Gly) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID163546 | Binding of Indolactam-V(ILV) to mutant Protein kinase C delta C1b domain (Phe13 to Gly) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID312193 | Selectivity ratio of PKCdelta C1B domain over PKCdelta C1B P11dfP mutant | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID312196 | Induction of GFP-tagged PKCalpha translocation in HeLa cells assessed as ratio of protein level in plasma membrane to cytosol at 1 uM | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID163670 | Ratio of binding to PKC delta C1b domain wild type and mutant (Leu20 to Gly) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID501080 | Induction of human HUES8 cell differentiation into pancreatic progenitor cell assessed as HNF6 expression in cells pregrown in medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic acid at 300 nM after 4 days by immunocytochemistry relative | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID321007 | Displacement of [3H]PDBu from PKCalpha C1A domain | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
| Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction. |
| AID232116 | Ratio of binding affinity to PKC delta C1b domain wild type versus mutant T12G | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID155882 | Displacement of [3H]PDBu from protein kinase C delta C1b domain mutant (L20G) | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID163679 | Displacement of [3H]- PDBu from Protein kinase C delta C1b domain | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
| Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V. |
| AID501105 | Induction of mouse AV3 cell differentiation into pancreatic lineage assessed as increase in Pdx-1 expression at 300 nM after 6 days by immunohistochemistry pretreated with 1000 ng/ml recombinant mouse Nodal for 5 days (Rvb = 4.0+/-1.5%) | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501072 | Induction of human HUES9 cell differentiation into pancreatic lineage assessed as increase in Pdx1-expression in cells pregrown with medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic acid at 1 uM after 4 days by Opera high content scree | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID163535 | Displacement of [3H]- PDBu from Protein kinase C delta C1a domain | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
| Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V. |
| AID155892 | Displacement of [3H]PDBu from protein kinase C delta C1b domain mutant (Q27G) (Not determined) | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID155894 | Displacement of [3H]PDBu from protein kinase C delta C1b domain mutant (W22G) (Not determined) | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID501091 | Induction of human HUES8 cell differentiation into pancreatic progenitor cell assessed as increase in NKX6.1 mRNA expression at 300 nM after 4 days by RT-PCR analysis cells pregrown in medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic a | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID80958 | Tested for epstein barr virus early antigen (EBV-EA) inducing activity in differentiated HL-60 cells at 10e-6 M | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID164207 | Displacement of [3H]- PDBu from Protein kinase C delta C1b domain | 2002 | Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
| Structural basis of RasGRP binding to high-affinity PKC ligands. |
| AID163543 | Binding of Indolactam-V(ILV) to mutant Protein kinase C delta C1b domain (Leu21 to Gly) (Not determined) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID1870486 | Inhibition of GLI in mouse NIH/3T3 cells assessed as reduction in CMV-driven firefly luciferase activity in starvation medium at 100 nM incubated for 30 hrs by Bright-Glo luciferase assay | 2022 | ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
| Indolactam Dipeptides as Nanomolar Gli Inhibitors. |
| AID164825 | Activation of partially purified HeLa cell protein kinase C, 32P incorporation into calf thymus histone(III-S). | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
| Synthesis of structural analogues of lyngbyatoxin A and their evaluation as activators of protein kinase C. |
| AID164186 | Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C theta C1b domain | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID155890 | Displacement of [3H]PDBu from protein kinase C delta C1b domain mutant (L21G) (Not determined) | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID501129 | Induction of AFP expression in CD1 nude mouse liver at 300 nM after 4 days by fluorescent confocal microscopy | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID163671 | Ratio of binding to PKC delta C1b domain wild type and mutant (Phe13 to Gly) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID82174 | Dose inducing HL-60 cell adhesion related to skin tumor promotion. | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12
| Active conformation of a tumor promoter, teleocidin. A molecular dynamics study. |
| AID501092 | Induction of insulin production in differentiated human HUES8 cells at 300 nM after 4 days by immunocytochemistry (Rvb = 0%) | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID164038 | Displacement of [3H]- PDBu from Protein kinase C gamma C1b domain | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
| Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V. |
| AID501112 | Induction of mouse AV3 cell differentiation into pancreatic lineage assessed as increase in Foxa2 mRNA expression at 300 nM after 6 days by RT-PCR analysis pretreated with 1000 ng/ml recombinant mouse Nodal for 5 days | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501116 | Induction of human HUES8 differentiation into definitive endoderm assessed as expression of SOX17 at 300 nM after 3 days by immunocytochemistry | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID312208 | Induction of GFP-tagged PKCdelta translocation in HeLa cells assessed as ratio of protein level in plasma membrane to cytosol at 1 uM | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID501126 | Induction of CDX2 expression in CD1 nude mouse intestine at 300 nM after 4 days by fluorescent confocal microscopy | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID163026 | Displacement of [3H]- PDBu from recombinant PKC alpha expressed in baculovirus | 1997 | Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
| Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivit |
| AID80962 | Tested for superoxide (O2-) generation inducing activity in differentiated HL-60 cells at 10e-6 M | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID501109 | Induction of mouse AV3 cell differentiation into pancreatic lineage assessed as increase in cdcp1 mRNA expression at 300 nM after 6 days by RT-PCR analysis pretreated with 1000 ng/ml recombinant mouse Nodal for 5 days | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID312183 | Displacement of [3H]PDBu from PKCbeta C1A domain | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID232108 | Ratio of binding affinity to PKC delta C1b domain wild type versus mutant F13G | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID163539 | Binding of Indolactam-V(ILV) to mutant Protein kinase C delta C1b domain (Gln27 to Trp) (Not determined) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID501111 | Induction of mouse AV3 cell differentiation into pancreatic lineage assessed as increase in Hnf6 mRNA expression at 300 nM after 6 days by RT-PCR analysis pretreated with 1000 ng/ml recombinant mouse Nodal for 5 days | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID163174 | Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C alpha C1a domain | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID155881 | Displacement of [3H]PDBu from protein kinase C delta C1b domain mutant (F13G) | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis. |
| AID163540 | Binding of Indolactam-V(ILV) to mutant Protein kinase C delta C1b domain (Gln27 to Val) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID1845950 | Reversal of HIV-1 latency in human ACH-2 cells assessed as increase in GFP positive cells incubated for 24 hrs by flow cytometry | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | HIV latency reversal agents: A potential path for functional cure? |
| AID501099 | Induction of C-peptide release in human HUES8 insulin-producing cell at 300 nM after 4 days by ELISA | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID321009 | Displacement of [3H]PDBu from PKCbeta C1A domain | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
| Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction. |
| AID501132 | Induction of SOX2 expression in CD1 nude mouse lung at 300 nM after 4 days by fluorescent confocal microscopy | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID163672 | Ratio of binding to PKC delta C1b domain wild type and mutant (Pro11 to Gly) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID501094 | Induction of C-peptide expression in human HUES8 insulin-producing cells at 300 nM after 4 days by immunocytochemistry relative to control | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501135 | Induction of desmin expression in CD1 nude mouse mesoderm at 300 nM after 4 days by fluorescent confocal microscopy | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501114 | Induction of cell proliferation in human HUES8 Pdx1 expressing cells assessed as expression of Ki67 at 300 nM after 4 days by immunocytochemistry | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID312184 | Displacement of [3H]PDBu from PKCbeta C1B domain | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID163176 | Displacement of [3H]- PDBu from Protein kinase C alpha C1a domain | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
| Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V. |
| AID501102 | Induction of human HUES8 differentiation into pancreatic lineage assessed as increase in DBA-positive exocrine cells at 300 nM after 4 days by RT-PCR (Rvb = 0.8+/-0.2%) | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID163024 | Displacement of phorbol 12,13-dibutyrate (PDBU) from recombinant Protein kinase C alpha | 1999 | Bioorganic & medicinal chemistry letters, May-17, Volume: 9, Issue:10
| Synthesis and protein kinase C binding activity of benzolactam-V7. |
| AID321010 | Displacement of [3H]PDBu from PKCalpha C1B domain | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
| Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction. |
| AID501117 | Induction of human GTE cells differentiation into pancreatic lineage assessed as increase in Pdx1-expressing cells at 300 nM after 4 days by immunocytochemistry pregrown in medium with FGF10 and KAAD-cyclopamine (Rvb (DMSO) = 2.8+/-0.6%) | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID163678 | Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C delta C1b domain | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID501085 | Induction of human HUES8 cell differentiation into pancreatic progenitor cell assessed as increase in PTF1A mRNA expression at 300 nM after 4 days by RT-PCR analysis cells pregrown in medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic ac | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID312212 | Induction of GFP-tagged PKCepsilon translocation in HeLa cells assessed as ratio of protein level in plasma membrane to cytosol at 1 uM | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID164033 | Displacement of [3H]- PDBu from Protein kinase C gamma C1a domain | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
| Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V. |
| AID312216 | Induction of GFP-tagged PKCeta translocation in HeLa cells assessed as ratio of protein level in plasma membrane to cytosol at 1 uM | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID501137 | Induction of nestin expression in CD1 nude mouse ectoderm at 300 nM after 4 days by fluorescent confocal microscopy | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID164032 | Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C gamma C1a domain | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID312186 | Displacement of [3H]PDBu from PKCgamma C1B domain | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID163534 | Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C delta C1a domain | 2001 | Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
| The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities. |
| AID501078 | Induction of human HUES4 cell differentiation into pancreatic progenitor cells assessed as increase in Pdx1-expression in cells pregrown with medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic acid at 300 nM after 4 days by Opera high co | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID163668 | Binding of Indolactam-V(ILV) to wild-type Protein kinase C delta C1b domain | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID163541 | Binding of Indolactam-V(ILV) to mutant Protein kinase C delta C1b domain (Leu20 to Gly) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID501127 | Induction of CES2 expression in CD1 nude mouse intestine at 300 nM after 4 days by fluorescent confocal microscopy | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID501077 | Induction of human HUES2 cell differentiation into pancreatic progenitor cells assessed as increase in Pdx1-expression in cells pregrown with medium containing Wnt, activin, FGF10, KAAD-cyclopamine and retinoic acid at 300 nM after 4 days by Opera high co | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID321014 | Displacement of [3H]PDBu from PKCepsilon C1B domain | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
| Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction. |
| AID501108 | Induction of mouse AV3 cell differentiation into pancreatic lineage assessed as increase in Pdx1 mRNA expression at 300 nM after 6 days by RT-PCR analysis pretreated with 1000 ng/ml recombinant mouse Nodal for 5 days | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID163837 | Displacement of [3H]- PDBu from recombinant PKC epsilon expressed in baculovirus | 1997 | Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
| Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivit |
| AID501138 | Induction of SOX1 expression in CD1 nude mouse ectoderm at 300 nM after 4 days by fluorescent confocal microscopy | 2009 | Nature chemical biology, Apr, Volume: 5, Issue:4
| A small molecule that directs differentiation of human ESCs into the pancreatic lineage. |
| AID312204 | Induction of GFP-tagged PKCgamma translocation in HeLa cells assessed as ratio of protein level in plasma membrane to cytosol at 1 uM | 2008 | Journal of medicinal chemistry, Jan-10, Volume: 51, Issue:1
| Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes. |
| AID163663 | Binding of Indolactam-V(ILV) to mutant Protein kinase C delta C1b domain (Pro11 to Gly) | 1999 | Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
| Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |