arcyriaflavin A: from marine ascidian, Eudistoma sp.; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 5327723 |
| CHEMBL ID | 268368 |
| CHEBI ID | 93276 |
| SCHEMBL ID | 8124103 |
| MeSH ID | M0237035 |
| Synonym |
|---|
| chembl268368 , |
| bdbm2672 |
| 3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^{11,15}.0^{17,22}]tricosa-1(16),2(10),4(9),5,7,11(15),17(22),18,20-nonaene-12,14-dione |
| 6,7,12,13-tetrahydro-5,7-dioxo-5h-indolo[2,3-a]pyrrolo[3,4-c]carbazole |
| HMS3269E19 |
| 12,13-dihydro-5h-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6h)-dione |
| BRD-K72726508-001-01-3 |
| 5h-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6h)-dione, 12,13-dihydro- |
| arcyriaflavin a |
| NCGC00159573-01 |
| HMS3229B05 |
| 118458-54-1 |
| SCHEMBL8124103 |
| DTXSID50416132 |
| AKOS024457112 |
| J-003757 |
| CHEBI:93276 |
| 12,13-dihydro-5h-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5 ,7(6h)-dione |
| BCP24907 |
| Q27164989 |
| lsm-3627 |
| FT-0701521 |
| HMS3677O10 |
| HMS3413O10 |
| arcyriaflavin-a |
| NCGC00159573-02 |
| 3,13,23-triazahexacyclo[14.7.0.02,10.04,9.011,15.017,22]tricosa-1,4,6,8,10,15,17,19,21-nonaene-12,14-dione |
| HY-103382 |
| CS-0027783 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| Class | Description |
|---|---|
| indolocarbazole | Compounds based upon an indolo[2,3-a]carbazole skeleton. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 8.9125 | 0.0020 | 14.6779 | 39.8107 | AID1476 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 5.6234 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 25.1189 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 31.6228 | 0.0316 | 22.3146 | 100.0000 | AID588579 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cyclin-T1 | Homo sapiens (human) | IC50 (µMol) | 20.0000 | 0.0010 | 0.5585 | 8.0000 | AID1513684 |
| Serine/threonine-protein kinase D3 | Homo sapiens (human) | IC50 (µMol) | 50.1550 | 0.0001 | 1.1701 | 10.0000 | AID155709; AID164952 |
| G2/mitotic-specific cyclin-B2 | Homo sapiens (human) | IC50 (µMol) | 1.1150 | 0.0025 | 1.8172 | 10.0000 | AID53345; AID55343 |
| G1/S-specific cyclin-E2 | Homo sapiens (human) | IC50 (µMol) | 0.8067 | 0.0010 | 1.7394 | 10.0000 | AID53835; AID55361; AID55363; AID55503 |
| cAMP-dependent protein kinase catalytic subunit alpha | Bos taurus (cattle) | IC50 (µMol) | 5.5129 | 0.0020 | 1.2409 | 9.0000 | AID1795412; AID1795945; AID1795948; AID1795971 |
| Epidermal growth factor receptor | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0000 | 0.5369 | 10.0000 | AID69403 |
| Protein kinase C gamma type | Homo sapiens (human) | IC50 (µMol) | 50.1550 | 0.0001 | 1.0354 | 10.0000 | AID155709; AID164952 |
| Protein kinase C beta type | Homo sapiens (human) | IC50 (µMol) | 66.7700 | 0.0001 | 0.5542 | 10.0000 | AID155709; AID164952 |
| Cyclin-dependent kinase 1 | Homo sapiens (human) | IC50 (µMol) | 0.8886 | 0.0004 | 1.3452 | 10.0000 | AID1513678; AID1795971; AID53345; AID55343 |
| Calcium/calmodulin-dependent protein kinase type II subunit alpha | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.6394 | 0.0001 | 0.7109 | 8.4000 | AID1795948; AID1795971 |
| Cyclin-dependent kinase 4 | Homo sapiens (human) | IC50 (µMol) | 1.5939 | 0.0006 | 0.5706 | 10.0000 | AID1513680; AID1795945; AID1795948; AID1795971; AID54031; AID55347; AID55348; AID55357; AID55359 |
| G2/mitotic-specific cyclin-B1 | Homo sapiens (human) | IC50 (µMol) | 0.8886 | 0.0013 | 1.4518 | 10.0000 | AID1513678; AID1795971; AID53345; AID55343 |
| Protein kinase C alpha type | Homo sapiens (human) | IC50 (µMol) | 48.3367 | 0.0001 | 0.9720 | 10.0000 | AID155709; AID164952; AID165134 |
| cAMP-dependent protein kinase catalytic subunit alpha | Homo sapiens (human) | IC50 (µMol) | 2.0000 | 0.0009 | 1.3241 | 9.0000 | AID164479; AID164482; AID164644 |
| Cyclin-A2 | Homo sapiens (human) | IC50 (µMol) | 0.1350 | 0.0004 | 1.0339 | 10.0000 | AID1513681 |
| cAMP-dependent protein kinase catalytic subunit gamma | Homo sapiens (human) | IC50 (µMol) | 2.0000 | 0.0009 | 1.5482 | 9.0000 | AID164479; AID164482; AID164644 |
| cAMP-dependent protein kinase catalytic subunit beta | Homo sapiens (human) | IC50 (µMol) | 2.0000 | 0.0006 | 1.4848 | 9.0000 | AID164479; AID164482; AID164644 |
| G1/S-specific cyclin-D1 | Homo sapiens (human) | IC50 (µMol) | 1.5939 | 0.0006 | 0.5479 | 9.5000 | AID1513680; AID1795945; AID1795948; AID1795971; AID54031; AID55347; AID55348; AID55357; AID55359 |
| Protein kinase C eta type | Homo sapiens (human) | IC50 (µMol) | 50.1550 | 0.0001 | 0.7971 | 10.0000 | AID155709; AID164952 |
| G1/S-specific cyclin-E1 | Homo sapiens (human) | IC50 (µMol) | 1.8697 | 0.0010 | 1.0404 | 10.0000 | AID1513679; AID1795945; AID1795948; AID1795971; AID53835; AID55361; AID55363; AID55503 |
| Cyclin-dependent kinase 2 | Homo sapiens (human) | IC50 (µMol) | 1.7677 | 0.0004 | 1.0444 | 10.0000 | AID1513679; AID1513681; AID1795945; AID1795948; AID1795971; AID53835; AID55361; AID55363; AID55503 |
| Protein kinase C iota type | Homo sapiens (human) | IC50 (µMol) | 50.1550 | 0.0001 | 2.0378 | 10.0000 | AID155709; AID164952 |
| Cyclin-dependent kinase 7 | Homo sapiens (human) | IC50 (µMol) | 20.0000 | 0.0001 | 0.9106 | 9.2000 | AID1513683 |
| Cyclin-dependent kinase 9 | Homo sapiens (human) | IC50 (µMol) | 20.0000 | 0.0010 | 0.6236 | 8.0000 | AID1513684 |
| Cyclin-H | Homo sapiens (human) | IC50 (µMol) | 20.0000 | 0.0005 | 1.0823 | 9.2000 | AID1513683 |
| CDK-activating kinase assembly factor MAT1 | Homo sapiens (human) | IC50 (µMol) | 20.0000 | 0.0030 | 1.6892 | 9.2000 | AID1513683 |
| Cyclin-dependent-like kinase 5 | Homo sapiens (human) | IC50 (µMol) | 0.9360 | 0.0002 | 1.1832 | 10.0000 | AID1513682 |
| Protein kinase C epsilon type | Homo sapiens (human) | IC50 (µMol) | 50.1550 | 0.0001 | 0.8029 | 10.0000 | AID155709; AID164952 |
| Protein kinase C theta type | Homo sapiens (human) | IC50 (µMol) | 34.2700 | 0.0001 | 0.9897 | 10.0000 | AID155709; AID164952; AID1678147 |
| Protein kinase C zeta type | Homo sapiens (human) | IC50 (µMol) | 50.1550 | 0.0001 | 2.4453 | 10.0000 | AID155709; AID164952 |
| Protein kinase C delta type | Homo sapiens (human) | IC50 (µMol) | 50.1550 | 0.0001 | 0.8448 | 10.0000 | AID155709; AID164952 |
| Calcium/calmodulin-dependent protein kinase type II subunit beta | Homo sapiens (human) | IC50 (µMol) | 0.0750 | 0.0001 | 1.0320 | 10.0000 | AID45962; AID45967 |
| Calcium/calmodulin-dependent protein kinase type II subunit gamma | Homo sapiens (human) | IC50 (µMol) | 0.0750 | 0.0004 | 1.0531 | 10.0000 | AID45962; AID45967 |
| Calcium/calmodulin-dependent protein kinase type II subunit delta | Homo sapiens (human) | IC50 (µMol) | 0.0750 | 0.0000 | 0.9157 | 10.0000 | AID45962; AID45967 |
| Cyclin-dependent kinase 5 activator 1 | Homo sapiens (human) | IC50 (µMol) | 0.9360 | 0.0010 | 1.2898 | 10.0000 | AID1513682 |
| Serine/threonine-protein kinase D1 | Homo sapiens (human) | IC50 (µMol) | 50.1550 | 0.0001 | 1.2319 | 10.0000 | AID155709; AID164952 |
| G2/mitotic-specific cyclin-B3 | Homo sapiens (human) | IC50 (µMol) | 1.1150 | 0.0025 | 1.8172 | 10.0000 | AID53345; AID55343 |
| cAMP-dependent protein kinase | Oryctolagus cuniculus (rabbit) | IC50 (µMol) | 10.0000 | 0.0000 | 0.0000 | 0.0000 | AID155691 |
| Calcium/calmodulin-dependent protein kinase type II subunit alpha | Homo sapiens (human) | IC50 (µMol) | 0.0750 | 0.0000 | 1.6395 | 10.0000 | AID45962; AID45967 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID55359 | Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 in enzymatic assay by measuring phosphorylation of RbING | 2003 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14 | Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles. |
| AID1513681 | Inhibition of GST-tagged CDK2/cyclin A2 (unknown origin) expressed in Escherichia coli using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID39106 | Antiproliferative activity against B16 mouse melanoma cells | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22 | Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties. |
| AID164640 | Inhibition of Protein Kinase A (PKA). | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22 | Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties. |
| AID80684 | In vitro antiproliferative activity against HCT116 ( human colon) cell line. | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides. |
| AID1513684 | Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID80381 | Inhibition of human HCT(colon) carcinoma cell proliferation | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. |
| AID54031 | Inhibitory activity against Cyclin-dependent kinase 4-cyclin D1 using Rb21 as substrate | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. |
| AID683929 | Inhibition of Protein kinase C gamma type at 10 uM by luciferase assay | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Testing the promiscuity of commercial kinase inhibitors against the AGC kinase group using a split-luciferase screen. |
| AID1513678 | Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID55503 | Inhibitory activity against Cyclin E-cyclin-dependent kinase 2 in enzymatic assay by measuring phosphorylation of RbING | 2003 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14 | Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles. |
| AID144793 | In vitro antiproliferative activity against NCI-460 (human lung) cell line. | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides. |
| AID164479 | Inhibition of Protein kinase A | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. |
| AID150379 | Antiproliferative activity against P388 Murine Leukemia cells | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22 | Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties. |
| AID69403 | Inhibitory activity against recombinant tyrosine kinase EGF-R (EGF-R ICD) | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7 | Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase. |
| AID164482 | Inhibition of Protein kinase A | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides. |
| AID164623 | Inhibition of Protein kinase A (Histone) (not tested) | 2003 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14 | Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles. |
| AID683919 | Inhibition of AKT1 at 10 uM by luciferase assay | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Testing the promiscuity of commercial kinase inhibitors against the AGC kinase group using a split-luciferase screen. |
| AID155691 | Inhibitory activity was determined against protein kinase A (PKA) of rabbit | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7 | Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase. |
| AID144788 | Flow cytometry proliferation assay in human lung NCI-460 cell line, G1 arrest | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides. |
| AID164644 | Inhibitory activity against Protein kinase A using histone as substrate | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. |
| AID143039 | Inhibition of human NCI-H460 (lung) carcinoma cell proliferation | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. |
| AID55363 | Inhibition of Cyclin E-cyclin-dependent kinase 2 | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. |
| AID45967 | Inhibitory activity against Calcium/calmodulin-dependent protein kinase type II using autocamtide as substrate | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. |
| AID683920 | Inhibition of AKT2 at 10 uM by luciferase assay | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Testing the promiscuity of commercial kinase inhibitors against the AGC kinase group using a split-luciferase screen. |
| AID1513682 | Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID90608 | Inhibitory activity against human cytomegalo virus (HCMV) using standard plaque reduction assay | 2001 | Bioorganic & medicinal chemistry letters, Aug-06, Volume: 11, Issue:15 | Synthesis of N-alkyl substituted indolocarbazoles as potent inhibitors of human cytomegalovirus replication. |
| AID1513679 | Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID56700 | Inhibitory activity towards Topoisomerase 1 from calf thymus. | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22 | Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties. |
| AID164952 | Inhibition of Protein kinase C | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. |
| AID45962 | Inhibition of Calcium/calmodulin-dependent protein kinase type II | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. |
| AID683921 | Inhibition of AKT3 at 10 uM by luciferase assay | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Testing the promiscuity of commercial kinase inhibitors against the AGC kinase group using a split-luciferase screen. |
| AID1513709 | Induction of cell cycle arrest in human HCT116 cells assessed as reduction in accumulation at G1 phase 1.25 to 20 uM after 24 hrs by propidium iodide-staining based flow cytometry | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID1513710 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase 1.25 to 20 uM after 24 hrs by propidium iodide-staining based flow cytometry relative to control | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID53835 | Inhibitory activity against Cyclin-dependent kinase 2-cyclin E using Rb21 as substrate | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. |
| AID55348 | Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 by measuring the phosphorylation of RbING | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. |
| AID55343 | Inhibition of Cyclin B-cyclin-dependent kinase 1 | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors. |
| AID55357 | Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 in enzymatic assay by measuring phosphorylation of Rb21 | 2003 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14 | Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles. |
| AID55347 | Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 by measuring phosphorylation of RbING substrate | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides. |
| AID218371 | Compound was evaluated for its cytotoxicity against Vero cell line | 2001 | Bioorganic & medicinal chemistry letters, Aug-06, Volume: 11, Issue:15 | Synthesis of N-alkyl substituted indolocarbazoles as potent inhibitors of human cytomegalovirus replication. |
| AID80509 | Flow cytometry proliferation assay in human colon HCT116 cell line, G1 arrest | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides. |
| AID55361 | Inhibitory activity against Cyclin E-cyclin-dependent kinase 2 by measuring phosphorylation of RbING substrate | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides. |
| AID78447 | In vitro antiproliferative activity against human carcinoma cell line HCT116 (colon) | 2003 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14 | Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles. |
| AID155709 | Inhibitory activity was determined against protein kinase C (PKC) from porcine brain | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7 | Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase. |
| AID1513683 | Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID165134 | Inhibition of Protein Kinase C(PKC) | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22 | Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties. |
| AID57052 | Inhibitory activity towards Topoisomerase 2 from calf thymus | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22 | Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties. |
| AID683927 | Inhibition of Protein kinase C delta type at 10 uM by luciferase assay | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Testing the promiscuity of commercial kinase inhibitors against the AGC kinase group using a split-luciferase screen. |
| AID1678146 | Inhibition of PKCtheta (unknown origin) at 2.5 ug/ml by HTRF assay relative to control | |||
| AID1513680 | Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID1678147 | Inhibition of PKCtheta (unknown origin) by HTRF assay | |||
| AID683928 | Inhibition of Protein kinase C epsilon type at 10 uM by luciferase assay | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Testing the promiscuity of commercial kinase inhibitors against the AGC kinase group using a split-luciferase screen. |
| AID40215 | Antimicrobial activity on Bacillus cereus | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22 | Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties. |
| AID78475 | Inhibition of cell growth of HCT116 tumor cell lines | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. |
| AID143205 | Inhibition of cell growth of NCI-H460 tumor cell lines | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. |
| AID74096 | Inhibitory activity against Glycogen synthase kinase-3 beta using pCREB as substrate; NA means Inactive at a concentration of 20 uM | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. |
| AID165290 | Percent inhibition of protein kinase C at 100 uM | 2001 | Bioorganic & medicinal chemistry letters, Aug-06, Volume: 11, Issue:15 | Synthesis of N-alkyl substituted indolocarbazoles as potent inhibitors of human cytomegalovirus replication. |
| AID78414 | In vitro antiproliferative activity against human carcinoma cell line H460 (lung) | 2003 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14 | Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles. |
| AID53345 | Inhibitory activity against Cyclin-dependent kinase 1-cyclin B using histone as substrate | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1795971 | Kinase Inhibition Assay from Article 10.1021/jm0256169: \\Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors.\\ | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. |
| AID1795948 | CDK Kinase Inhibition Assay from Article 10.1016/s0960-894x(03)00461-x: \\Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.\\ | 2003 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14 | Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles. |
| AID1795945 | CDK Kinase Inhibition Assay from Article 10.1016/S0960-894X(03)00792-3: \\Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides.\\ | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides. |
| AID1795412 | PKC assay from Article : \\The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.\\ | 1991 | The Journal of biological chemistry, Aug-25, Volume: 266, Issue:24 | The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 5 (19.23) | 18.2507 |
| 2000's | 8 (30.77) | 29.6817 |
| 2010's | 7 (26.92) | 24.3611 |
| 2020's | 6 (23.08) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (21.99) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 26 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||