| Assay ID | Title | Year | Journal | Article |
|---|
| AID1289201 | Binding affinity to PB1 bromodomain5 (unknown origin) by isothermal titration calorimetric analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors. |
| AID1289204 | Binding affinity to PB1 bromodomain5 (unknown origin) at 10 uM by DFS analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors. |
| AID1308372 | Half life in PBS at pH 7.4 at 20 degC | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1886342 | Binding affinity to human PBRM1 bromodomain 5 (S645 to D766 residues) expressed in bacterial expression system by bromoscan assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. |
| AID1888674 | Anti-tumor activity against human MT330 cells xenografted in NSG mouse assessed as reduction in tumor growth at 10 mg/kg, ip for alterate days combination with TMZ and measured after 8 weeks | 2022 | Bioorganic & medicinal chemistry, 01-01, Volume: 53 | Novel structural-related analogs of PFI-3 (SRAPs) that target the BRG1 catalytic subunit of the SWI/SNF complex increase the activity of temozolomide in glioblastoma cells. |
| AID1310276 | Binding affinity to His6-tagged human recombinant PB1 bromodomain isoform 5 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by VP-ITC microcalorimetry | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex. |
| AID1308388 | Drug recovery in cell media after 1 week at 37 degC by HPLC analysis | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1683141 | Binding affinity to polybromo-1 (1) (unknown origin) assessed as change in melting temperature at 20 uM by SYPRO orange dye based DSF assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1308370 | Binding affinity to human PB1 isoform 5 expressed in BL21 (DE3)-R3-BirA cells by isothermal titration calorimetry | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1888670 | Antiproliferative activity against human LN-229 cells assessed as reduction in cell viability at 2 uM up to 7 days by incucyte live cell assay | 2022 | Bioorganic & medicinal chemistry, 01-01, Volume: 53 | Novel structural-related analogs of PFI-3 (SRAPs) that target the BRG1 catalytic subunit of the SWI/SNF complex increase the activity of temozolomide in glioblastoma cells. |
| AID1886340 | Binding affinity to human SMARCA4 (A1448 to S1575 residues) expressed in bacterial expression system by bromoscan assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. |
| AID1308364 | Binding affinity to human PB1 isoform 4 expressed in BL21 (DE3)-R3-BirA cells assessed as change in melting temperature at 10 uM by sypro-orange dye-based differential scanning fluorimetric analysis | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1289200 | Binding affinity to SMARCA4 (unknown origin) by isothermal titration calorimetric analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors. |
| AID1886338 | Inhibition of BRD4 bromodomain 1 (unknown origin) by TR-FRET assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. |
| AID1888672 | Binding affinity to epitope-tagged BRG1 bromodomain (unknown origin) expressed in MT330 cells assessed as thermostability at < 54.2 degC at 30 uM for 2 hrs by CESTA | 2022 | Bioorganic & medicinal chemistry, 01-01, Volume: 53 | Novel structural-related analogs of PFI-3 (SRAPs) that target the BRG1 catalytic subunit of the SWI/SNF complex increase the activity of temozolomide in glioblastoma cells. |
| AID1308380 | Cytotoxicity against mouse C2C12 cells assessed as cell death at 100 uM after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1310275 | Binding affinity to His6-tagged human recombinant PB1 bromodomain isoform 5 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells assessed as change in melting temperature at 10 uM by SyproOrange dye based DSF thermal shift assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex. |
| AID1888673 | Anti-tumor activity against human MT330 cells xenografted in NSG mouse assessed as reduction in tumor growth at 10 mg/kg, ip for alterate days combination with TMZ and measured after 2 weeks | 2022 | Bioorganic & medicinal chemistry, 01-01, Volume: 53 | Novel structural-related analogs of PFI-3 (SRAPs) that target the BRG1 catalytic subunit of the SWI/SNF complex increase the activity of temozolomide in glioblastoma cells. |
| AID1308367 | Binding affinity to human SMARC2B expressed in BL21 (DE3)-R3-BirA cells assessed as change in melting temperature at 10 uM by sypro-orange dye-based differential scanning fluorimetric analysis | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1683118 | Inhibition of IBMX/insulin/dexamethasone/rosiglitazone-induced adipocyte differentiation in mouse 3T3-L1 cells assessed as effect on lipid droplet accumulation at 5 uM incubated for 14 days by oil red O staining | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1289202 | Binding affinity to SMARCA2 (unknown origin) at 10 uM by DFS analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors. |
| AID1888671 | Antiproliferative activity against human LN-229 cells assessed as reduction in cell viability at 2 uM combination with TMZ up to 7 days by incucyte live cell assay | 2022 | Bioorganic & medicinal chemistry, 01-01, Volume: 53 | Novel structural-related analogs of PFI-3 (SRAPs) that target the BRG1 catalytic subunit of the SWI/SNF complex increase the activity of temozolomide in glioblastoma cells. |
| AID1886343 | Binding affinity to human PBRM1 bromodomain 2 (S178 to E291 residues) expressed in bacterial expression system by bromoscan assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. |
| AID1308365 | Binding affinity to human PB1 isoform 5 expressed in BL21 (DE3)-R3-BirA cells assessed as change in melting temperature at 10 uM by sypro-orange dye-based differential scanning fluorimetric analysis | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1886341 | Binding affinity to human SMARCA2 (S1337 to Q1486 residues) expressed in bacterial expression system by bromoscan assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. |
| AID1886336 | Inhibition of SMARCA2 (unknown origin) by TR-FRET assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. |
| AID1308386 | Inhibition of differentiation of mouse C3H10T1/2 cells to adipocytes assessed as lipid accumulation at 20 uM by oil red O staining-based assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1308381 | Cytotoxicity against mouse C3H10T1/2 cells assessed as cell death at 100 uM after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1308368 | Binding affinity to human SMARCA4 expressed in BL21 (DE3)-R3-BirA cells assessed as change in melting temperature at 10 uM by sypro-orange dye-based differential scanning fluorimetric analysis | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1308362 | Binding affinity to human PB1 isoform 2 expressed in BL21 (DE3)-R3-BirA cells assessed as change in melting temperature at 10 uM by sypro-orange dye-based differential scanning fluorimetric analysis | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1308377 | Antiproliferative activity against human RCC4 cells at 0.1 to 10 uM incubated for 24 to 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1310278 | Binding affinity to His6-tagged human recombinant SMARCA4 bromodomain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by VP-ITC microcalorimetry | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex. |
| AID1308363 | Binding affinity to human PB1 isoform 3 expressed in BL21 (DE3)-R3-BirA cells assessed as change in melting temperature at 10 uM by sypro-orange dye-based differential scanning fluorimetric analysis | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1308371 | Binding affinity to human SMARCA4 expressed in BL21 (DE3)-R3-BirA cells by isothermal titration calorimetry | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1683135 | Binding affinity to SMARCA2 (unknown origin) assessed as change in melting temperature at 20 uM by SYPRO orange dye based DSF assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1888666 | Induction of cell death in human MT330 cells assessed as reduction in cell viability at 2 uM after 3 days by ELISA | 2022 | Bioorganic & medicinal chemistry, 01-01, Volume: 53 | Novel structural-related analogs of PFI-3 (SRAPs) that target the BRG1 catalytic subunit of the SWI/SNF complex increase the activity of temozolomide in glioblastoma cells. |
| AID1683136 | Binding affinity to polybromo-1 (6) (unknown origin) assessed as change in melting temperature at 20 uM by SYPRO orange dye based DSF assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1683138 | Binding affinity to polybromo-1 (5) (unknown origin) assessed as change in melting temperature at 20 uM by SYPRO orange dye based DSF assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1683134 | Binding affinity to SMARCA4 (unknown origin) assessed as change in melting temperature at 20 uM by SYPRO orange dye based DSF assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1308379 | Cytotoxicity against mouse C3H10T1/2 cells assessed as cell viability up to 50 uM after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1683110 | Inhibition of IBMX/insulin/dexamethasone/rosiglitazone-induced adipocyte differentiation in mouse 3T3-L1 cells assessed as reduction in C/EBPalpha mRNA expression at 5 uM incubated for 14 days by qPCR analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1308378 | Cytotoxicity against mouse C2C12 cells assessed as cell viability up to 50 uM after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1683111 | Inhibition of IBMX/insulin/dexamethasone/rosiglitazone-induced adipocyte differentiation in mouse 3T3-L1 cells assessed as reduction in PPARgamma mRNA expression at 5 uM incubated for 14 days by qPCR analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1308382 | Inhibition of differentiation in mouse C2C12 cells assessed as suppression of MyHC expression at 1 uM by HRP-peroxidase-based immunocytochemistry | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1308366 | Binding affinity to human SMARC2A expressed in BL21 (DE3)-R3-BirA cells assessed as change in melting temperature at 10 uM by sypro-orange dye-based differential scanning fluorimetric analysis | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1308384 | Inhibition of differentiation of mouse C3H10T1/2 cells to adipocytes assessed as lipid accumulation at 1 uM by oil red O staining-based assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1289203 | Binding affinity to SMARCA4 (unknown origin) at 10 uM by DFS analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors. |
| AID1886337 | Inhibition of PBRM1 bromodomain 5 (unknown origin) by TR-FRET assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. |
| AID1886335 | Inhibition of His-tagged SMARCA4 (unknown origin) (1448 to 1575 residues) using biotinylated ARTKQTARKSTGG-K(Ac)-APR-K(Ac)-QLAT-K(Ac)-AAR-K(Ac)-SAPGG-K as substrate incubated for 10 mins by TR-FRET assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. |
| AID1310277 | Binding affinity to His6-tagged human recombinant SMARCA4 bromodomain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells assessed as change in melting temperature at 10 uM by SyproOrange dye based DSF thermal shift assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex. |
| AID1683140 | Binding affinity to polybromo-1 (2) (unknown origin) assessed as change in melting temperature at 20 uM by SYPRO orange dye based DSF assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1886339 | Binding affinity to His6/FLAG-tagged SMARCA4 (unknown origin) by isothermal titration calorimetric assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. |
| AID1886344 | Inhibition of SMARAC2 isoform B (unknown origin) expressed in U2OS cells co-expressed in NLS-ZsGreen incubated for 1 hrs by cellular target engagement assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. |
| AID1308361 | Inhibition of differentiation in mouse C2C12 cells assessed as shortening of myotubes with lower nuclei at 500 nM to 50 uM by HRP-peroxidase-based immunocytochemistry relative to control | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1683139 | Binding affinity to polybromo-1 (3) (unknown origin) assessed as change in melting temperature at 20 uM by SYPRO orange dye based DSF assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1888668 | Induction of cell death in human MT330 cells assessed as reduction in cell viability at 2 uM combination with TMZ after 3 days by ELISA | 2022 | Bioorganic & medicinal chemistry, 01-01, Volume: 53 | Novel structural-related analogs of PFI-3 (SRAPs) that target the BRG1 catalytic subunit of the SWI/SNF complex increase the activity of temozolomide in glioblastoma cells. |
| AID1308376 | Antiproliferative activity against human 786-0 cells at 0.1 to 10 uM incubated for 24 to 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
| Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
| AID1683109 | Inhibition of IBMX/insulin/dexamethasone/rosiglitazone-induced adipocyte differentiation in mouse 3T3-L1 cells assessed as reduction in FABP4 mRNA expression at 5 uM incubated for 14 days by qPCR analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1683137 | Binding affinity to polybromo-1 (4) (unknown origin) assessed as change in melting temperature at 20 uM by SYPRO orange dye based DSF assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |