| Assay ID | Title | Year | Journal | Article |
|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1233038 | 1-Octanol-aqueous phosphate buffer partition coefficient, logD of the compound at pH 7.4 | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
| Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2. |
| AID1392785 | Total plasma clearance in rat at 3 mg/kg, iv or 10 mg/kg, po | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1547109 | Inhibition of ERK5 (unknown origin) at 1 uM by Z'-Lyte assay relative to control | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Discovery of a Novel Dual-Target Inhibitor of ERK1 and ERK5 That Induces Regulated Cell Death to Overcome Compensatory Mechanism in Specific Tumor Types. |
| AID1482243 | Inhibition of ERK2 in human A375 cells harboring BRAF V600E mutant assessed as decrease in phosphorylated ERK2 levels | 2017 | Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
| Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point. |
| AID1392794 | Inhibition of CYP3A4 (unknown origin) under pre-incubation condition | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1392793 | Oral bioavailability in dog at 10 mg/kg | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1233037 | Inhibition of MEK1 (unknown origin) autophosphorylation incubated with enzyme for 20 mins prior to ATP addition by ADP Glo kinase assay in presence of ATP at Km concentration | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
| Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2. |
| AID1385283 | Clearance in dog hepatocytes assessed per million cells | | | |
| AID1233036 | Antiproliferative activity against human A375 cells harboring B-RAF V600E mutant after 72 hrs by Cellomics ArrayScanTM VTI imaging analysis | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
| Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2. |
| AID1626509 | Solubility in human FaSSIF at pH 6.5 | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery of 1-(1H-Pyrazolo[4,3-c]pyridin-6-yl)urea Inhibitors of Extracellular Signal-Regulated Kinase (ERK) for the Treatment of Cancers. |
| AID1527709 | Binding affinity to MEK-activated phosphorylated biotinylated ERK2 (unknown origin) assessed as dissociation rate constant by SPR analysis | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC). |
| AID1385284 | Apparent permeability in human Caco2 cells | | | |
| AID1385292 | Half life in dog | | | |
| AID1385275 | Inhibition of ERK2 (unknown origin) using peptide substrate measured after 45 mins by IMAP assay | | | |
| AID1385293 | Mean residence time in dog | | | |
| AID1392784 | Apparent permeability in human Caco2 cells assessed per 10'6 cells | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1233034 | Inhibition of ERK2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-ERK2 level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
| Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2. |
| AID1547125 | Inhibition of ERK5 in human MKN74 cells harboring ERK1/2 siRNA assessed as reduction in ERK5 phosphorylation at 1 uM by Western blot analysis | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Discovery of a Novel Dual-Target Inhibitor of ERK1 and ERK5 That Induces Regulated Cell Death to Overcome Compensatory Mechanism in Specific Tumor Types. |
| AID1385280 | Inhibition of human ERG at 1.5 mg/ml by binding assay relative to control | | | |
| AID1233035 | Inhibition of ERK1/2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-RSK level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
| Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2. |
| AID1547110 | Antiproliferative activity against human HL60 cells assessed as reduction in cell viability measured after 24 hrs | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Discovery of a Novel Dual-Target Inhibitor of ERK1 and ERK5 That Induces Regulated Cell Death to Overcome Compensatory Mechanism in Specific Tumor Types. |
| AID1385276 | Antiproliferative activity against human HT-29 cells harboring BRAF V600E/D mutant measured after 4 days | | | |
| AID1896215 | Inhibition of ERK1 (unknown origin) incubated for 45 mins in presence of ATP by IMAP assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Targeting Extracellular Signal-Regulated Protein Kinase 1/2 (ERK1/2) in Cancer: An Update on Pharmacological Small-Molecule Inhibitors. |
| AID1385281 | Inhibition of human ERG at 5 mg/ml by binding assay relative to control | | | |
| AID1385286 | Plasma clearance in rat | | | |
| AID1527707 | Binding affinity to MEK-activated phosphorylated biotinylated ERK2 (unknown origin) assessed as association rate constant by SPR analysis | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC). |
| AID1233032 | Inhibition of MEK U911-activated ERK2 (unknown origin) using Erktide as substrate preincubated with enzyme for 20 mins prior to substrate addition by RapidFire Mass Spectrometry in presence of ATP at Km concentration | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
| Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2. |
| AID1547108 | Inhibition of ERK2 (unknown origin) at 1 uM by Z'-Lyte assay relative to control | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Discovery of a Novel Dual-Target Inhibitor of ERK1 and ERK5 That Induces Regulated Cell Death to Overcome Compensatory Mechanism in Specific Tumor Types. |
| AID1392803 | Induction of apoptosis in human HT-29 cells harboring BRAF/KRAS mutant by caspase activation assay | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1392782 | Clearance in dog hepatocytes assessed per million cells | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1392780 | Inhibition of human ERG at 1.5 mg/ml by Rb efflux assay | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1385289 | Oral bioavailability in rat | | | |
| AID1392788 | Oral bioavailability in rat at or 10 mg/kg | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1527705 | Binding affinity to MEK-activated phosphorylated biotinylated ERK2 (unknown origin) by SPR analysis | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC). |
| AID1385288 | Mean residence time in rat | | | |
| AID1697359 | Binding affinity to recombinant wild-type ERK3 (9 to 327 residues) (unknown origin) expressed in Escherichia coli by microscale thermophoresis assay | 2020 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
| Biochemical, cellular and structural characterization of novel and selective ERK3 inhibitors. |
| AID1896216 | Inhibition of ERK2 (unknown origin) incubated for 45 mins in presence of ATP by IMAP assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Targeting Extracellular Signal-Regulated Protein Kinase 1/2 (ERK1/2) in Cancer: An Update on Pharmacological Small-Molecule Inhibitors. |
| AID1392792 | MRT in dog at 2 mg/kg, iv or 2 mg/kg dosed via portal vein infusion or 10 mg/kg, po | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1626508 | Antiproliferative activity against human A375SM cells harboring BRAF V600E mutant measured after 96 hrs by Cell Titer-Glo assay | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery of 1-(1H-Pyrazolo[4,3-c]pyridin-6-yl)urea Inhibitors of Extracellular Signal-Regulated Kinase (ERK) for the Treatment of Cancers. |
| AID1392787 | MRT in rat at 3 mg/kg, iv or 10 mg/kg, po | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1848246 | Antiproliferative activity against human RBE cells overexpressing Hh/ERK pathway assessed as inhibition of cell growth incubated for 96 hrs by CCK8 assay | 2022 | Bioorganic & medicinal chemistry, 11-15, Volume: 74 | Design, synthesis and biological evaluation of novel 4-aminopiperidine derivatives as SMO/ERK dual inhibitors. |
| AID1392781 | Inhibition of human ERG at 5 mg/ml by Rb efflux assay | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1547111 | Antiproliferative activity against human MKN74 cells assessed as reduction in cell viability measured after 24 hrs | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Discovery of a Novel Dual-Target Inhibitor of ERK1 and ERK5 That Induces Regulated Cell Death to Overcome Compensatory Mechanism in Specific Tumor Types. |
| AID1233039 | Solubility of the compound in aqueous phosphate buffer at 25 degC at pH 7.4 after 24 hrs | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
| Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2. |
| AID1385290 | AUC in dog at 10 mg/kg | | | |
| AID1527706 | Binding affinity to non-phosphorylated biotinylated ERK2 (unknown origin) assessed as association rate constant by SPR analysis | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC). |
| AID1527683 | Inhibition of ERK1/2 in human A375 cells assessed as inhibition of ERK phosphorylation after 2 hrs | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC). |
| AID1392770 | Oral bioavailability in rat at 10 mg/kg | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1385274 | Inhibition of ERK1 (unknown origin) using peptide substrate measured after 45 mins by IMAP assay | | | |
| AID1392768 | Inhibition of ERK2 (unknown origin) preincubated for 45 mins followed by substrate addition measured after 0.5 hrs by IMAP assay | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1233033 | Inhibition of MEK U911-activated ERK2 (unknown origin) using Erktide as substrate preincubated with enzyme for 20 mins prior to substrate addition by RapidFire Mass Spectrometry in presence of ATP at higher concentration | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
| Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2. |
| AID1626506 | Inhibition of ERK (unknown origin) assessed as inhibition of RSK phosphorylation | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery of 1-(1H-Pyrazolo[4,3-c]pyridin-6-yl)urea Inhibitors of Extracellular Signal-Regulated Kinase (ERK) for the Treatment of Cancers. |
| AID1482248 | Inhibition of MEK1 (unknown origin) | 2017 | Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
| Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point. |
| AID1527684 | Inhibition of ERK1/2 in human A375 cells assessed as inhibition of RSK phosphorylation after 2 hrs | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC). |
| AID1392769 | AUC in rat at 10 mg/kg | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1626507 | Inhibition of MEK in human A375 cells assessed as inhibition of ERK phosphorylation | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery of 1-(1H-Pyrazolo[4,3-c]pyridin-6-yl)urea Inhibitors of Extracellular Signal-Regulated Kinase (ERK) for the Treatment of Cancers. |
| AID1385277 | Antiproliferative activity against human COLO205 cells harboring BRAF V600E/D mutant measured after 4 days | | | |
| AID1527704 | Binding affinity to non-phosphorylated biotinylated ERK2 (unknown origin) by SPR analysis | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC). |
| AID1392789 | AUC in dog at 10 mg/kg, po | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1247141 | Inhibition of ERK2 (unknown origin) after 45 mins by IMAP assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Recent progress on MAP kinase pathway inhibitors. |
| AID1547112 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Discovery of a Novel Dual-Target Inhibitor of ERK1 and ERK5 That Induces Regulated Cell Death to Overcome Compensatory Mechanism in Specific Tumor Types. |
| AID1527708 | Binding affinity to non-phosphorylated biotinylated ERK2 (unknown origin) assessed as dissociation rate constant by SPR analysis | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC). |
| AID1392791 | Half life in dog at at 2 mg/kg, iv or 2 mg/kg dosed via portal vein infusion or 10 mg/kg, po | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1392779 | Inhibition of CYP3A4 (unknown origin) under co-incubation condition | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1392790 | Total plasma clearance in dog at 2 mg/kg, iv or 2 mg/kg dosed via portal vein infusion or 10 mg/kg, po | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1848242 | Inhibition of SMO in mouse 3T3/HH FlashII-7 cells incubated for 36 hrs in presence of SHH by Gli-luciferase reporter assay | 2022 | Bioorganic & medicinal chemistry, 11-15, Volume: 74 | Design, synthesis and biological evaluation of novel 4-aminopiperidine derivatives as SMO/ERK dual inhibitors. |
| AID1385282 | Clearance in human hepatocytes assessed per million cells | | | |
| AID1527710 | Binding affinity to non-phosphorylated biotinylated ERK2 (unknown origin) assessed as mean residence time by measuring half life by SPR analysis | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC). |
| AID1547107 | Inhibition of ERK1 (unknown origin) at 1 uM by Z'-Lyte assay relative to control | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
| Discovery of a Novel Dual-Target Inhibitor of ERK1 and ERK5 That Induces Regulated Cell Death to Overcome Compensatory Mechanism in Specific Tumor Types. |
| AID1385291 | Plasma clearance in dog | | | |
| AID1626505 | Inhibition of human ERK2 preincubated for 15 mins followed by addition of IMAP peptide substrate and ATP measured after 60 mins by IMAP-FP assay | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| Discovery of 1-(1H-Pyrazolo[4,3-c]pyridin-6-yl)urea Inhibitors of Extracellular Signal-Regulated Kinase (ERK) for the Treatment of Cancers. |
| AID1385285 | AUC in rat at 10 mg/kg | | | |
| AID1385278 | Inhibition of CYP3A4 (unknown origin) co-incubated with substrate | | | |
| AID1527711 | Binding affinity to MEK-activated phosphorylated biotinylated ERK2 (unknown origin) assessed as mean residence time by measuring half life by SPR analysis | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC). |
| AID1392786 | Half life in rat at 3 mg/kg, iv or 10 mg/kg, po | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1697358 | Binding affinity to wild-type human partial length ERK3 (M1 to P413 residues) expressed in bacterial expression system at 1 uM by kinomescan method relative to control | 2020 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
| Biochemical, cellular and structural characterization of novel and selective ERK3 inhibitors. |
| AID1247140 | Inhibition of ERK1 (unknown origin) after 45 mins by IMAP assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Recent progress on MAP kinase pathway inhibitors. |
| AID1482244 | Inhibition of ERK2 in human A375 cells harboring BRAF V600E mutant assessed as decrease in phosphorylated RSK levels | 2017 | Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
| Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point. |
| AID1848245 | Inhibition of ERK2 (unknown origin) using kinase substrate 8 at 100 nM incubated for 40 mins in presence of ATP by mobility shift assay | 2022 | Bioorganic & medicinal chemistry, 11-15, Volume: 74 | Design, synthesis and biological evaluation of novel 4-aminopiperidine derivatives as SMO/ERK dual inhibitors. |
| AID1385294 | Oral bioavailability in dog | | | |
| AID1385279 | Inhibition of CYP3A4 (unknown origin) preincubated followed by substrate addition | | | |
| AID1392783 | Clearance in human hepatocytes assessed per million cells | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| AID1385287 | Half life in rat | | | |
| AID1392778 | Antiproliferative activity against human HT-29 cells harboring BRAF/KRAS mutant | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
| Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology. |
| 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. |
| AID1345344 | Human mitogen-activated protein kinase 1 (ERK subfamily) | 2013 | Cancer discovery, Jul, Volume: 3, Issue:7
| Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |