Harmine: Alkaloid isolated from seeds of PEGANUM HARMALA; ZYGOPHYLLACEAE. It is identical to banisterine, or telepathine, from Banisteria caapi and is one of the active ingredients of hallucinogenic drinks made in the western Amazon region from related plants. It has no therapeutic use, but (as banisterine) was hailed as a cure for postencephalitic PARKINSON DISEASE in the 1920's. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
harmine : A harmala alkaloid in which the harman skeleton is methoxy-substituted at C-7. [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]
| Flora | Rank | Flora Definition | Family | Family Definition |
|---|---|---|---|---|
| Peganum | genus | A plant genus of the family ZYGOPHYLLACEAE. HARMALINE and other ALKALOIDS, phenylpropanoids, and TRITERPENES have been found in plants of this genus.[MeSH] | Nitrariaceae | [no description available] |
| ID Source | ID |
|---|---|
| PubMed CID | 5280953 |
| CHEMBL ID | 269538 |
| CHEMBL ID | 4095474 |
| CHEBI ID | 28121 |
| SCHEMBL ID | 292955 |
| MeSH ID | M0009805 |
| Synonym |
|---|
| BIDD:GT0106 |
| BIDD:ER0478 |
| brn 0178813 |
| yageine |
| 1-methyl-7-methoxy-beta-carboline |
| telepathine |
| banisterine |
| leucoharmine |
| einecs 207-131-4 |
| 9h-pyrido(3,4-b)indole, 7-methoxy-1-methyl- |
| 7-methoxy-1-methyl-9h-pyrido(3,4-b)indole |
| yajeine |
| smr001233259 |
| MLS002153910 , |
| BRD-K30984264-003-03-5 |
| BRD-K30984264-001-04-7 |
| DIVK1C_006707 |
| SDCCGMLS-0066733.P001 |
| SPECTRUM_001128 |
| NCGC00016435-01 |
| cas-343-27-1 |
| OPREA1_596686 |
| PRESTWICK2_000613 |
| ACON0_001194 |
| PRESTWICK3_000613 |
| ACON1_000061 |
| MEGXP0_001875 |
| SPECTRUM5_001914 |
| inchi=1/c13h12n2o/c1-8-13-11(5-6-14-8)10-4-3-9(16-2)7-12(10)15-13/h3-7,15h,1-2h |
| 9h-pyrido[3,4-b]indole, 7-methoxy-1-methyl- |
| 7-methoxy-1-methyl-9h-beta-carboline |
| 7-methoxy-1-methyl-9h-pyrido[3,4-b]indole |
| AB00052850 |
| C06538 |
| harmine |
| 442-51-3 |
| harmine, 98% |
| NCGC00094869-05 |
| NCGC00094869-02 |
| NCGC00094869-01 |
| NCGC00094869-03 |
| KBIO2_001608 |
| KBIO2_006744 |
| KBIO1_001651 |
| KBIOSS_001608 |
| KBIOGR_001467 |
| KBIO2_004176 |
| KBIO3_001852 |
| SPECTRUM2_000568 |
| SPECTRUM4_001004 |
| PRESTWICK0_000613 |
| SPECPLUS_000611 |
| SPECTRUM3_000906 |
| PRESTWICK1_000613 |
| SPBIO_002765 |
| SPBIO_000356 |
| SPECTRUM1500867 |
| BPBIO1_000602 |
| BSPBIO_000546 |
| NCGC00094869-06 |
| NCGC00094869-04 |
| HRM , |
| H-1200 |
| harmin hydrochloride |
| STK047386 |
| NCGC00016435-09 |
| HMS2090H04 |
| DB07919 |
| AKOS003673313 |
| chebi:28121 , |
| CHEMBL269538 |
| H0001 |
| HMS1921M06 |
| BRD-K30984264-003-06-8 |
| 7-methoxy-1-methylbeta-carboline |
| A826517 |
| S3868 |
| CCG-38734 |
| NCGC00016435-06 |
| NCGC00016435-02 |
| NCGC00016435-04 |
| NCGC00016435-07 |
| NCGC00016435-03 |
| NCGC00016435-05 |
| BRD-K30984264-001-05-4 |
| unii-4fhh5g48t7 |
| 5-23-12-00237 (beilstein handbook reference) |
| 4fhh5g48t7 , |
| FT-0626860 |
| BRD-K30984264-001-01-3 |
| harmine [mart.] |
| harmine [mi] |
| BP-30211 |
| SCHEMBL292955 |
| 3ANR |
| AB00052850-08 |
| HY-N0737A |
| CS-5325 |
| yagein |
| 1-methyl-7-methoxy-.beta.-carboline |
| banisterin |
| telepathin |
| 7-methoxy-1-methyl-9h-beta-carboline # |
| harmin |
| bdbm100152 |
| cid_5359389 |
| 7-methoxy-1-methyl-9h-beta-carboline;hydrochloride |
| HMS3561B11 |
| gtpl9352 |
| AC-31456 |
| HMS3650H03 |
| mfcd00004958 |
| A1-03319 |
| DTXSID30196066 |
| SR-05000001527-4 |
| SR-05000001527-5 |
| sr-05000001527 |
| SR-05000001527-1 |
| 1-methyl-7-methoxy-beta -carboline |
| telepathien |
| garmin |
| 7-methoxy-1-methyl-9h-pyrido[3,4-b]indole, 9ci |
| 442-51-3 (free base) |
| 7-methoxy-1-methyl-9h-pyrido[3,4-b]indol; harmine |
| 122992-92-1 |
| AS-13970 |
| SR-05000001527-8 |
| Q128381 |
| HMS3885E10 |
| CHEMBL4095474 |
| harmine (telepathine) |
| SY062283 |
Harmine is a dual-specificity tyrosine-regulated kinase 1A (DYRK1A) inhibitor that displays a number of biological and pharmacological properties. It was recently shown to be able to induce degradation of Twist Family BHLH Transcription Factor 1 (Twist1) in non-small cell lung cancer cells (NSCLC)
Harmine has many pharmacological activities including anti-inflammatory, neuroprotective, antidiabetic, and antitumor activities. Harmine has been demonstrated to cause DNA damage by intercalating DNA.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Harmine has been demonstrated to cause DNA damage by intercalating DNA." | ( Harmine-based dual inhibitors targeting histone deacetylase (HDAC) and DNA as a promising strategy for cancer therapy. Chen, X; Cui, N; Ji, L; Kong, L; Li, S; Liu, X; Lu, D; Luo, H; Luo, Z; Peng, W; Qu, L; Wang, C; Wang, X; Yin, F, 2022) | 2.89 |
| "Harmine has many pharmacological activities including anti-inflammatory, neuroprotective, antidiabetic, and antitumor activities." | ( Pharmacological effects of harmine and its derivatives: a review. Li, D; Yu, S; Zhang, L, 2020) | 1.58 |
| "Harmine has various types of pharmacological activities such as antimicrobial, antifungal, antitumor, cytotoxic, antiplasmodial, antioxidaant, antimutagenic, antigenotoxic and hallucinogenic properties." | ( A review on medicinal importance, pharmacological activity and bioanalytical aspects of beta-carboline alkaloid ''Harmine''. Gadewar, M; Patel, DK; Patel, K; Prasad, SK; Tripathi, R, 2012) | 1.31 |
| "Harmine has various types of pharmacological activities including antimicrobial, antiplasmodial, antioxidative, antitumor, antimutagenic, antidiabetic, vasorelaxant and central excitation properties." | ( [Progress in study on effect of harmine on bone and cartilage metabolism]. Hu, Y; Xie, H, 2016) | 1.44 |
| "Harmine has antitumor and antinociceptive effects, and inhibits human DNA topoisomerase. " | ( Harmine induces apoptosis in HepG2 cells via mitochondrial signaling pathway. Cao, MR; Jiang, JW; Li, Q; Liao, XL; Liu, HH; Liu, ZL; Pan, YL; Wang, W, 2011) | 3.25 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Harmine did not inhibit P-glycoprotein (P-gp) mediated drug efflux." | ( The beta-carboline alkaloid harmine inhibits BCRP and can reverse resistance to the anticancer drugs mitoxantrone and camptothecin in breast cancer cells. Ma, Y; Wink, M, 2010) | 1.38 |
Harmine treatment (20mg/kg) prevented reductions in brain-derived neurotrophic factor (BDNF) protein levels and hippocampal neurogenesis induced by CUS. Harmine treatment effectively inhibited cell proliferation and induced the G1/S cell cycle arrest of NSCLC cells.
| Excerpt | Reference | Relevance |
|---|---|---|
| " Objective This study investigates the dynamic metabolic profiles and pharmacokinetic properties of harmane and its metabolites in rats in vivo." | ( Pharmacokinetic study of harmane and its 10 metabolites in rat after intravenous and oral administration by UPLC-ESI-MS/MS. Cheng, X; Jiang, B; Li, S; Liu, W; Teng, L; Wang, CH; Wang, Z, 2016) | 0.43 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The present study was performed to investigate whether three amino compounds, 1-methyl-9H-pyrido[3,4-b]indole (harman), 9H-pyrido[3,4-b]indole (norharman) and 2-amino-1,3,4-triazole (amitrole), might be converted in vivo to compounds capable of promoting hepatocarcinogenesis when given with NaNO(2)." | ( Lack of combination hepatocarcinogenicity of harman, norharman and amitrole when given with NaNO2 in the rat. Asamoto, M; Hirose, M; Ichihara, T; Imaida, K; Kawabe, M; Miyashita, K; Ogiso, T; Shirai, T; Tamano, S, 2005) | 0.33 |
| " The present study was an evaluation of proliferation, cytotoxicity and differentiation of harmine and harmaline on HL60 cells, alone or in combination with ATRA and G-CSF." | ( A study on the antitumoral and differentiation effects of peganum harmala derivatives in combination with ATRA on leukaemic cells. Arjmand, A; Oody, A; Zaker, F, 2007) | 0.56 |
| " The chromatographic fingerprints combined with PCA, HCA and LDA could distinguish the seeds of the different species of Peganum investigated." | ( HPLC fingerprints combined with principal component analysis, hierarchical cluster analysis and linear discriminant analysis for the classification and differentiation of Peganum sp. indigenous to China. Bligh, SW; Cheng, XM; Wang, CH; Wang, ZT; Yang, T; Zhao, T, ) | 0.13 |
| " In order to know whether harmane is extensively metabolized, a rapid and sensitive method using ultra-performance liquid chromatography combined with electrospray ionization quadrupole time-of-flight tandem mass spectrometry (UPLC/ESI-QTOF-MS) was used to analyze the metabolic profile of harmane in vitro and in vivo in rats." | ( Metabolites identification of harmane in vitro/in vivo in rats by ultra-performance liquid chromatography combined with electrospray ionization quadrupole time-of-flight tandem mass spectrometry. Cheng, X; Li, S; Liu, W; Teng, L; Wang, C; Wang, Z, 2014) | 0.4 |
| " The aims of the present study were therefore to determine whether norharmane, a tobacco constituent and monoamine oxidase inhibitor, is self-administered alone and/or in combination with nicotine, and to evaluate the neural mechanisms underlying acquisition of self-administration of the two drugs." | ( Reinforcing and neural activating effects of norharmane, a non-nicotine tobacco constituent, alone and in combination with nicotine. Arnold, MM; Belluzzi, JD; Leslie, FM; Loughlin, SE, 2014) | 0.4 |
Harmine exhibited dosage dependent (0, 5, 10, 20, 40, 80, 160, and 320 μmol/L) toxic effect. Growth inhibition, egg laying defects, shortened life span and increased mortality.
| Excerpt | Relevance | Reference |
|---|---|---|
| "In order to test the GABA hypothesis of kindling, GABA-complex antagonists were administered in a dose-response paradigm to rats that had been implanted with indwelling forebrain electrodes, but not kindled." | ( Secondary generalization in non-kindled rats following acute administration of GABA-complex and adenosine antagonists. Burnham, WM; Mingo, NS, 1990) | 0.28 |
| " At the higher dosage of harmol, phorone reduced the biliary excretion of harmol sulfate while increasing the biliary excretion of harmol glucuronide." | ( Effect of glutathione depletion on sulfate activation and sulfate ester formation in rats. Gregus, Z; Howell, S; Klaassen, CD; White, C, 1988) | 0.27 |
| " beta CCE and beta CCtB produced dose-related, parallel shifts in the dose-response curve for the discriminative effects of diazepam, but the magnitude of the shifts was limited: the two highest doses of beta CCE and beta CCtB produced shifts that were not significantly different in magnitude." | ( Beta-carbolines as antagonists of the discriminative stimulus effects of diazepam in rats. Cook, JA; Guzman, F; Hagen, TJ; Shannon, HE, 1988) | 0.27 |
| " Tremorolytic potency (ED50) was calculated from dose-response curves." | ( Cholecystokinin octapeptide (CCK-8), ceruletide and analogues of ceruletide: effects on tremors induced by oxotremorine, harmine and ibogaine. A comparison with prolyl-leucylglycine amide (MIF), anti-Parkinsonian drugs and clonazepam. Zetler, G, 1983) | 0.47 |
| " In the present study we determined the time-course and dose-response effects of 6-MeO-THbetaC for blockade of AGS." | ( Effects of 6-methoxy-1,2,3,4-tetrahydro-beta-carboline (6-MeO-THbetaC) on audiogenic seizures in DBA/2J mice. Buckholtz, NS; Sparks, DL, 1980) | 0.26 |
| " These findings indicate that harman affects the activity of mesolimbic dopaminergic neurons following a U-shaped dose-response relationship." | ( Harman-induced changes of extracellular concentrations of neurotransmitters in the nucleus accumbens of rats. Baum, SS; Hill, R; Rommelspacher, H, 1996) | 0.29 |
| " This is an illustration of the potential of PET to monitor drug effects directly on target biochemical systems in the brain in human volunteers, and the possibility of using these data, rather than pharmacokinetic data, for the determination of dosing intervals." | ( MAO-A inhibition in brain after dosing with esuprone, moclobemide and placebo in healthy volunteers: in vivo studies with positron emission tomography. Bergström, M; Eckernäs, SA; Grahnér, A; Greger, G; Gross, G; Långström, B; Müller-Peltzer, H; Németh, G; Safer, A; Traut, M; Westerberg, G, 1997) | 0.3 |
| "min/l after oral dosing of 7 and 65 microg/kg, respectively." | ( Pharmacokinetics of the beta-carboline norharman in man. Bom, I; Fekkes, D; Pepplinkhuizen, L; Tuiten, A, 2001) | 0.31 |
| " On the other hand, concentrations in the micromolar range that are reached in high dosage animal experiments with HA may well influence cytochrome activity and, thus, influence the experimental outcome of these studies." | ( Modulation of cytochrome P450 1A1 by food-derived heterocyclic aromatic amines. Hümmerich, J; Pfau, W; Zohm, C, 2004) | 0.32 |
| " We investigated the influence of dosing time on the neurotoxicity, nephrotoxicity, and immunosuppressive effect of tacrolimus in rats." | ( Tacrolimus-induced neurotoxicity and nephrotoxicity is ameliorated by administration in the dark phase in rats. Kataoka, Y; Oishi, R; Yamauchi, A, 2004) | 0.32 |
| ", fast and slow metabolizers of harmine-in 14 experienced male members of the União do Vegetal (UDV) who received a standardized dosage of hoasca." | ( Fast and slow metabolizers of Hoasca. Callaway, JC, 2005) | 0.61 |
| " Dose-response curves were determined for phenylephrine and for several imidazoline ligands, using endothelium denuded, isolated ring segments, of tail arteries from adult male Sprague-Dawley rats." | ( Centrally acting imidazolines stimulate vascular alpha 1A-adrenergic receptors in Rat-Tail Artery. Crane, L; Edwards, LP; George, OK; Gonzalez, RR; Kennedy, WB, ) | 0.13 |
| " Melatonin and AMK (10(-11)-10(-3) m), but not AFMK, inhibited nNOS activity in vitro in a dose-response manner." | ( Inhibition of neuronal nitric oxide synthase activity by N1-acetyl-5-methoxykynuramine, a brain metabolite of melatonin. Acuña-Castroviejo, D; Camacho, E; Carrión, MD; Entrena, A; Escames, G; Espinosa, A; Gallo, MA; León, J; López, LC; Reiter, RJ; Rodríguez, MI; Tan, DX; Tapias, V, 2006) | 0.33 |
| "The role of Mrp2, Bcrp, and P-glycoprotein in the biliary excretion of acetaminophen sulfate (AS) and glucuronide (AG), 4-methylumbelliferyl sulfate (4MUS) and glucuronide (4MUG), and harmol sulfate (HS) and glucuronide (HG) was studied in Abcc2(-/-), Abcg2(-/-), and Abcb1a(-/-)/Abcb1b(-/-) mouse livers perfused with the respective parent compounds using a cassette dosing approach." | ( The important role of Bcrp (Abcg2) in the biliary excretion of sulfate and glucuronide metabolites of acetaminophen, 4-methylumbelliferone, and harmol in mice. Brouwer, KL; Kalvass, JC; Nezasa, K; Patel, NJ; Raub, TJ; Tian, X; Zamek-Gliszczynski, MJ, 2006) | 0.33 |
| " In the present study, the involvement in this process of Mrp3 and Mrp4, two basolateral efflux transporters, was evaluated by analyzing the hepatic basolateral excretion of the glucuronide and sulfate metabolites of acetaminophen, 4-methylumbelliferone, and harmol in Abcc3(-/-) and Abcc4(-/-) mice using a cassette dosing approach." | ( Evaluation of the role of multidrug resistance-associated protein (Mrp) 3 and Mrp4 in hepatic basolateral excretion of sulfate and glucuronide metabolites of acetaminophen, 4-methylumbelliferone, and harmol in Abcc3-/- and Abcc4-/- mice. Belinsky, MG; Bridges, AS; Brouwer, KL; Kruh, GD; Lee, K; Nezasa, K; Tian, X; Zamek-Gliszczynski, MJ, 2006) | 0.33 |
| "For new MAO-A inhibitors, about 74% occupancy at steady-state dosing is desirable." | ( Monoamine oxidase A inhibitor occupancy during treatment of major depressive episodes with moclobemide or St. John's wort: an [11C]-harmine PET study. Houle, S; Meyer, JH; Parkes, J; Rusjan, P; Sacher, J; Sagrati, S; Wilson, AA, 2011) | 0.57 |
| " The in vivo assay was done on 60 experimentally infected pigeons dosed with metronidazole at 50 mg/kg body weight (BW) or alkaloids at 25 mg/kg BW." | ( Antitrichomonal activity of Peganum harmala alkaloid extract against trichomoniasis in pigeon (Columba livia domestica). Moghadamnia, AA; Tabari, MA; Youssefi, MR, 2017) | 0.46 |
| " elegans) as a model system, we found that harmine exhibited dosage dependent (0, 5, 10, 20, 40, 80, 160, and 320 μmol/L) toxic effect, such as growth inhibition, egg laying defects, shortened life span and increased mortality." | ( A preliminary study on the neurotoxic mechanism of harmine in Caenorhabditis elegans. Fang, Y; Fu, J; Jiang, K; Kong, C; Liu, C; Liu, Y; Sun, Q, 2021) | 1.14 |
| Role | Description |
|---|---|
| metabolite | Any intermediate or product resulting from metabolism. The term 'metabolite' subsumes the classes commonly known as primary and secondary metabolites. |
| anti-HIV agent | An antiviral agent that destroys or inhibits the replication of the human immunodeficiency virus. |
| EC 1.4.3.4 (monoamine oxidase) inhibitor | An EC 1.4.3.* (oxidoreductase acting on donor CH-NH2 group, oxygen as acceptor) inhibitor that interferes with the action of monoamine oxidase (EC 1.4.3.4). |
| [role 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] | |
| Class | Description |
|---|---|
| harmala alkaloid | Any member of a class of naturally occurring alkaloids based on a 1-methyl-9H-beta-carboline 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] | |
| Pathway | Proteins | Compounds |
|---|---|---|
| beta-carboline biosynthesis | 0 | 9 |
| beta-carboline biosynthesis | 0 | 8 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 20.4723 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 17.8524 | 0.0251 | 20.2376 | 39.8107 | AID893 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 17.8524 | 0.0251 | 20.2376 | 39.8107 | AID893 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 20.7706 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 39.8107 | 0.0020 | 14.6779 | 39.8107 | AID1476 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 56.2341 | 0.1000 | 20.8793 | 79.4328 | AID588456 |
| TDP1 protein | Homo sapiens (human) | Potency | 8.8562 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| Smad3 | Homo sapiens (human) | Potency | 35.4813 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 17.1125 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 6.3096 | 0.0013 | 7.7625 | 44.6684 | AID914; AID915 |
| 67.9K protein | Vaccinia virus | Potency | 18.6649 | 0.0001 | 8.4406 | 100.0000 | AID720579; AID720580 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 7.9433 | 0.0020 | 7.5337 | 39.8107 | AID891 |
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 18.1905 | 0.0018 | 15.6638 | 39.8107 | AID894 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 89.1251 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 23.1093 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 50.1187 | 0.1337 | 25.4129 | 89.1251 | AID588795 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 20.0809 | 0.0079 | 8.2332 | 1,122.0200 | AID2546; AID2551 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 3.3552 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 21.8865 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
| dual specificity protein kinase CLK4 | Homo sapiens (human) | Potency | 0.0671 | 0.0116 | 3.7867 | 31.6228 | AID1970 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 15.8489 | 0.2512 | 15.8432 | 39.8107 | AID504327 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 21.8865 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 15.8489 | 0.3162 | 12.7657 | 31.6228 | AID881 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 21.8865 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 21.8865 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 21.8865 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 21.8865 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 21.8865 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 21.8865 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 21.8865 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 21.8865 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 21.8865 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 21.8865 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 15.8489 | 0.0063 | 8.2350 | 39.8107 | AID881 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 21.8865 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 21.8865 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 21.8865 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 21.8865 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 21.8865 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| [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) |
|---|---|---|---|---|---|---|---|
| Chain A, Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Homo sapiens (human) | IC50 (µMol) | 0.3500 | 0.3500 | 0.3500 | 0.3500 | AID977608 |
| 5-hydroxytryptamine receptor 3E | Homo sapiens (human) | Ki | 10.0000 | 0.0010 | 0.8835 | 9.9000 | AID5996 |
| Glycogen synthase kinase-3 beta | Sus scrofa (pig) | IC50 (µMol) | 12.2500 | 0.0050 | 1.8419 | 10.0000 | AID1335820; AID1467090; AID707501; AID721735 |
| [Tau protein] kinase | Sus scrofa (pig) | IC50 (µMol) | 12.2500 | 0.0050 | 1.9832 | 10.0000 | AID1335820; AID1467090; AID707501; AID721735 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0002 | 0.6561 | 10.0000 | AID39935 |
| Histone deacetylase 3 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0004 | 0.6196 | 10.0000 | AID1266808; AID1415637; AID1622954 |
| Dual specificity protein kinase CLK2 | Mus musculus (house mouse) | IC50 (µMol) | 0.2800 | 0.1300 | 0.5800 | 2.1000 | AID707688 |
| Dual specificity protein kinase CLK3 | Mus musculus (house mouse) | IC50 (µMol) | 10.0000 | 1.2000 | 3.6800 | 6.4000 | AID707687 |
| Dual specificity protein kinase CLK4 | Mus musculus (house mouse) | IC50 (µMol) | 0.0500 | 0.0150 | 0.0944 | 0.6200 | AID707686 |
| Acetylcholinesterase | Electrophorus electricus (electric eel) | IC50 (µMol) | 16.4950 | 0.0000 | 0.9453 | 9.9400 | AID1900710; AID656680 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 3 | Homo sapiens (human) | IC50 (µMol) | 0.6040 | 0.0114 | 0.7859 | 3.2000 | AID1420028; AID1441344; AID435334; AID707506; AID721729 |
| Cyclin-T1 | Homo sapiens (human) | IC50 (µMol) | 0.7200 | 0.0010 | 0.5585 | 8.0000 | AID707692 |
| Serine/threonine-protein kinase D3 | Homo sapiens (human) | IC50 (µMol) | 250.0000 | 0.0001 | 1.1701 | 10.0000 | AID165278 |
| G2/mitotic-specific cyclin-B2 | Homo sapiens (human) | IC50 (µMol) | 18.0000 | 0.0025 | 1.8172 | 10.0000 | AID51723 |
| 5-hydroxytryptamine receptor 3B | Homo sapiens (human) | Ki | 10.0000 | 0.0010 | 0.8711 | 9.9000 | AID5996 |
| Protein kinase C gamma type | Homo sapiens (human) | IC50 (µMol) | 250.0000 | 0.0001 | 1.0354 | 10.0000 | AID165278 |
| Protein kinase C beta type | Homo sapiens (human) | IC50 (µMol) | 250.0000 | 0.0001 | 0.5542 | 10.0000 | AID165278 |
| Tyrosine-protein kinase Lck | Homo sapiens (human) | IC50 (µMol) | 250.0000 | 0.0002 | 1.3173 | 10.0000 | AID224133 |
| Tyrosine-protein kinase Fyn | Homo sapiens (human) | IC50 (µMol) | 250.0000 | 0.0002 | 1.6789 | 8.6800 | AID72269 |
| Cyclin-dependent kinase 1 | Homo sapiens (human) | IC50 (µMol) | 18.0000 | 0.0004 | 1.3452 | 10.0000 | AID51723 |
| Beta-2 adrenergic receptor | Homo sapiens (human) | Ki | 10.0000 | 0.0000 | 0.6635 | 9.5499 | AID41506 |
| Tyrosine-protein kinase Lyn | Homo sapiens (human) | IC50 (µMol) | 250.0000 | 0.0002 | 0.5594 | 5.2000 | AID224144 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Ki | 10.0000 | 0.0000 | 0.6902 | 10.0000 | AID142901 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | Ki | 10.0000 | 0.0000 | 0.7951 | 9.1201 | AID142901 |
| Beta-1 adrenergic receptor | Homo sapiens (human) | Ki | 10.0000 | 0.0001 | 1.3391 | 9.9840 | AID40566 |
| 5-hydroxytryptamine receptor 1A | Homo sapiens (human) | Ki | 10.0000 | 0.0001 | 0.5326 | 10.0000 | AID3824 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | Ki | 10.0000 | 0.0000 | 0.7292 | 6.9183 | AID142901 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 6.2700 | 0.0001 | 0.8074 | 10.0000 | AID35941; AID36487 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | Ki | 10.0000 | 0.0000 | 0.5972 | 9.1201 | AID142901 |
| Serine/threonine-protein kinase pim-1 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0004 | 0.8871 | 10.0000 | AID707500 |
| D(2) dopamine receptor | Homo sapiens (human) | Ki | 10.0000 | 0.0000 | 0.6518 | 10.0000 | AID63034 |
| G2/mitotic-specific cyclin-B1 | Homo sapiens (human) | IC50 (µMol) | 18.0000 | 0.0013 | 1.4518 | 10.0000 | AID51723 |
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | Ki | 7.7900 | 0.0001 | 0.6017 | 10.0000 | AID5536 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0002 | 0.6561 | 10.0000 | AID39935 |
| Protein kinase C alpha type | Homo sapiens (human) | IC50 (µMol) | 250.0000 | 0.0001 | 0.9720 | 10.0000 | AID165278 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 1.1300 | 0.0002 | 0.7257 | 10.0000 | AID36222 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0002 | 0.6561 | 10.0000 | AID39935 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0002 | 0.5614 | 10.0000 | AID39935 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | Ki | 0.8100 | 0.0003 | 0.4834 | 10.0000 | AID36400 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0002 | 0.6352 | 10.0000 | AID39935 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0002 | 0.6217 | 10.0000 | AID39935 |
| Cyclin-A2 | Homo sapiens (human) | IC50 (µMol) | 25.0000 | 0.0004 | 1.0339 | 10.0000 | AID1467084; AID53689; AID707695 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | Ki | 10.0000 | 0.0000 | 0.5405 | 7.7600 | AID142901 |
| Amine oxidase [flavin-containing] A | Homo sapiens (human) | IC50 (µMol) | 0.0044 | 0.0000 | 2.3789 | 9.7700 | AID1851169; AID1896381; AID1917481 |
| Amine oxidase [flavin-containing] A | Homo sapiens (human) | Ki | 0.0152 | 0.0019 | 2.3797 | 10.0000 | AID223242; AID453494; AID550168; AID611923 |
| D(1A) dopamine receptor | Homo sapiens (human) | Ki | 10.0000 | 0.0001 | 0.8363 | 10.0000 | AID63034 |
| D(4) dopamine receptor | Homo sapiens (human) | Ki | 10.0000 | 0.0000 | 0.4362 | 10.0000 | AID63034 |
| D(1B) dopamine receptor | Homo sapiens (human) | Ki | 10.0000 | 0.0003 | 0.4017 | 7.9000 | AID63034 |
| Dual specificity protein kinase CLK1 | Mus musculus (house mouse) | IC50 (µMol) | 0.0720 | 0.0080 | 0.5127 | 4.3000 | AID707702 |
| Metabotropic glutamate receptor 1 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0079 | 0.3145 | 0.9000 | AID108345 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0002 | 0.6758 | 10.0000 | AID39935 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0002 | 0.6469 | 10.0000 | AID39935 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | Ki | 3.2600 | 0.0003 | 1.4656 | 10.0000 | AID145367 |
| Protein kinase C eta type | Homo sapiens (human) | IC50 (µMol) | 250.0000 | 0.0001 | 0.7971 | 10.0000 | AID165278 |
| Cyclin-dependent kinase 2 | Homo sapiens (human) | IC50 (µMol) | 25.0000 | 0.0004 | 1.0444 | 10.0000 | AID1467084; AID53689; AID707695 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | Ki | 0.8100 | 0.0000 | 0.3609 | 10.0000 | AID36400 |
| Amine oxidase [flavin-containing] B | Homo sapiens (human) | Ki | 60.4110 | 0.0006 | 1.7771 | 10.0000 | AID223242; AID550169 |
| 5-hydroxytryptamine receptor 1D | Homo sapiens (human) | Ki | 10.0000 | 0.0001 | 0.8087 | 10.0000 | AID4616 |
| 5-hydroxytryptamine receptor 1B | Homo sapiens (human) | Ki | 10.0000 | 0.0001 | 0.5485 | 9.2100 | AID4247 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 9.3400 | 0.0001 | 0.9549 | 10.0000 | AID5615 |
| Neuromedin-B receptor | Homo sapiens (human) | Ki | 10.0000 | 0.0002 | 0.0008 | 0.0020 | AID4247 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0002 | 0.6561 | 10.0000 | AID39935 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0002 | 0.6561 | 10.0000 | AID39935 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0002 | 0.6712 | 10.0000 | AID39935 |
| Alpha-2B adrenergic receptor | Mus musculus (house mouse) | Ki | 10.0000 | 0.0002 | 0.1091 | 2.1500 | AID36487 |
| Metabotropic glutamate receptor 2 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0031 | 0.1265 | 0.4760 | AID108345 |
| Metabotropic glutamate receptor 3 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0030 | 0.1340 | 0.4760 | AID108345 |
| Metabotropic glutamate receptor 4 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.1600 | 1.7800 | 3.4000 | AID108345 |
| Metabotropic glutamate receptor 5 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0005 | 0.1964 | 3.7600 | AID108345 |
| Sodium-dependent serotonin transporter | Homo sapiens (human) | Ki | 10.0000 | 0.0000 | 0.7048 | 8.1930 | AID204092 |
| 5-hydroxytryptamine receptor 7 | Homo sapiens (human) | Ki | 5.5000 | 0.0003 | 0.3806 | 10.0000 | AID6591 |
| Alpha-1A adrenergic receptor | Homo sapiens (human) | Ki | 3.8733 | 0.0000 | 0.2726 | 10.0000 | AID36400; AID36487 |
| Alpha-1B adrenergic receptor | Homo sapiens (human) | Ki | 5.4050 | 0.0000 | 0.4713 | 10.0000 | AID36400; AID37207 |
| Metabotropic glutamate receptor 7 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.1100 | 0.1100 | 0.1100 | AID108345 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 10.0000 | 0.0000 | 0.6020 | 10.0000 | AID63034 |
| Kappa-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 5.0360 | 0.0003 | 0.7123 | 7.0700 | AID707693; AID707702 |
| Protein kinase C iota type | Homo sapiens (human) | IC50 (µMol) | 250.0000 | 0.0001 | 2.0378 | 10.0000 | AID165278 |
| 5-hydroxytryptamine receptor 3A | Homo sapiens (human) | Ki | 10.0000 | 0.0000 | 0.7411 | 9.9000 | AID5996 |
| 5-hydroxytryptamine receptor 5A | Homo sapiens (human) | Ki | 10.0000 | 0.0008 | 0.9433 | 5.1600 | AID6482; AID6500 |
| Casein kinase I isoform delta | Homo sapiens (human) | IC50 (µMol) | 1.5000 | 0.0040 | 1.1272 | 10.0000 | AID1330646; AID435450 |
| Casein kinase I isoform epsilon | Homo sapiens (human) | IC50 (µMol) | 1.5000 | 0.0040 | 1.1150 | 9.5000 | AID1330646 |
| Dual specificity protein kinase CLK1 | Homo sapiens (human) | IC50 (µMol) | 0.0860 | 0.0074 | 0.4344 | 2.1000 | AID1284866; AID1330649; AID1335822; AID721732 |
| Glycogen synthase kinase-3 alpha | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0010 | 1.2249 | 9.1000 | AID1165916; AID1330647; AID707503 |
| Glycogen synthase kinase-3 beta | Homo sapiens (human) | IC50 (µMol) | 24.0333 | 0.0006 | 0.8013 | 10.0000 | AID1165916; AID1330647; AID1648105; AID1765289; AID1900714; AID707502 |
| 5-hydroxytryptamine receptor 6 | Homo sapiens (human) | Ki | 1.4800 | 0.0002 | 0.5229 | 10.0000 | AID6517 |
| Cyclin-dependent kinase 7 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0001 | 0.9106 | 9.2000 | AID707693 |
| Cyclin-dependent kinase 9 | Homo sapiens (human) | IC50 (µMol) | 0.7200 | 0.0010 | 0.6236 | 8.0000 | AID707692 |
| Cyclin-H | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0005 | 1.0823 | 9.2000 | AID707693 |
| Histone deacetylase 4 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0006 | 1.0526 | 10.0000 | AID1266808; AID1415637; AID1622954 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0002 | 0.5577 | 10.0000 | AID39935 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0002 | 0.6403 | 10.0000 | AID39935 |
| Mitogen-activated protein kinase 1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 30.0000 | 0.0020 | 0.0818 | 0.2200 | AID707504 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0002 | 0.5708 | 10.0000 | AID39935 |
| Metabotropic glutamate receptor 8 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1.9000 | 2.6500 | 3.4000 | AID108345 |
| Cyclin-A1 | Homo sapiens (human) | IC50 (µMol) | 32.5000 | 0.0005 | 1.4715 | 10.0000 | AID53689; AID707695 |
| Cholinesterase | Equus caballus (horse) | IC50 (µMol) | 13.6000 | 0.0000 | 2.2214 | 9.4000 | AID1900711 |
| Cyclin-dependent-like kinase 5 | Homo sapiens (human) | IC50 (µMol) | 11.4000 | 0.0002 | 1.1832 | 10.0000 | AID1165915; AID1335819; AID54179; AID707694; AID721736 |
| Alpha-2C adrenergic receptor | Mus musculus (house mouse) | Ki | 10.0000 | 0.0002 | 0.1091 | 2.1500 | AID36487 |
| Alpha-2A adrenergic receptor | Mus musculus (house mouse) | Ki | 10.0000 | 0.0002 | 0.1091 | 2.1500 | AID36487 |
| Protein kinase C epsilon type | Homo sapiens (human) | IC50 (µMol) | 250.0000 | 0.0001 | 0.8029 | 10.0000 | AID165278 |
| Protein kinase C theta type | Homo sapiens (human) | IC50 (µMol) | 250.0000 | 0.0001 | 0.9897 | 10.0000 | AID165278 |
| Protein kinase C zeta type | Homo sapiens (human) | IC50 (µMol) | 250.0000 | 0.0001 | 2.4453 | 10.0000 | AID165278 |
| Protein kinase C delta type | Homo sapiens (human) | IC50 (µMol) | 250.0000 | 0.0001 | 0.8448 | 10.0000 | AID165278 |
| Aldehyde oxidase | Homo sapiens (human) | IC50 (µMol) | 0.0300 | 0.0023 | 0.6320 | 3.3000 | AID653127 |
| Histone deacetylase 1 | Homo sapiens (human) | IC50 (µMol) | 5.5000 | 0.0001 | 0.5543 | 9.9000 | AID1266808; AID1403152; AID1415637; AID1543929; AID1578886; AID1622954 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Homo sapiens (human) | IC50 (µMol) | 0.0917 | 0.0031 | 0.7140 | 9.0120 | AID1062364; AID1165914; AID1203148; AID1237105; AID1284862; AID1284956; AID1330648; AID1335821; AID1335828; AID1356537; AID1356538; AID1420021; AID1420026; AID1420029; AID1441342; AID1478836; AID1546958; AID1714121; AID1752117; AID1820103; AID1823462; AID1851170; AID1882232; AID435570; AID653127; AID697228; AID707509; AID707683; AID721731 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Homo sapiens (human) | Ki | 0.0330 | 0.0100 | 0.4108 | 1.5000 | AID752777 |
| Cyclin-dependent kinase 5 activator 1 | Homo sapiens (human) | IC50 (µMol) | 11.4000 | 0.0010 | 1.2898 | 10.0000 | AID1165915; AID1335819; AID54179; AID707694; AID721736 |
| Serine/threonine-protein kinase D1 | Homo sapiens (human) | IC50 (µMol) | 250.0000 | 0.0001 | 1.2319 | 10.0000 | AID165278 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0397 | 0.0100 | 0.5741 | 2.8000 | AID707684; AID707685; AID721733 |
| 5-hydroxytryptamine receptor 3D | Homo sapiens (human) | Ki | 10.0000 | 0.0010 | 0.8835 | 9.9000 | AID5996 |
| Serine/threonine-protein kinase pim-3 | Homo sapiens (human) | IC50 (µMol) | 4.3000 | 0.0001 | 0.4198 | 4.3000 | AID435577 |
| Serine/threonine-protein kinase haspin | Homo sapiens (human) | IC50 (µMol) | 0.5900 | 0.0020 | 0.1907 | 0.7700 | AID655305 |
| Histone deacetylase 7 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0007 | 1.0260 | 9.9000 | AID1266808; AID1415637; AID1622954 |
| G2/mitotic-specific cyclin-B3 | Homo sapiens (human) | IC50 (µMol) | 18.0000 | 0.0025 | 1.8172 | 10.0000 | AID51723 |
| 5-hydroxytryptamine receptor 3C | Homo sapiens (human) | Ki | 10.0000 | 0.0010 | 0.8835 | 9.9000 | AID5996 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0002 | 0.6561 | 10.0000 | AID39935 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 2 | Homo sapiens (human) | IC50 (µMol) | 1.3137 | 0.0140 | 0.9744 | 3.0000 | AID1203150; AID1284864; AID1420027; AID1441343; AID435571; AID653129; AID707507; AID721730 |
| Histone deacetylase 2 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0001 | 0.7221 | 9.9700 | AID1266808; AID1415637; AID1622954 |
| Polyamine deacetylase HDAC10 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0005 | 0.7245 | 9.9000 | AID1266808; AID1415637; AID1622954 |
| Histone deacetylase 11 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0003 | 0.9298 | 9.9000 | AID1266808; AID1415637; AID1622954 |
| Histone deacetylase 8 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0007 | 0.9947 | 9.9000 | AID1266808; AID1415637; AID1622954 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0002 | 0.6561 | 10.0000 | AID39935 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 4 | Homo sapiens (human) | IC50 (µMol) | 54.5000 | 0.5200 | 4.8000 | 9.5000 | AID1203151; AID1441346; AID707505 |
| Histone deacetylase 6 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 0.5376 | 9.9000 | AID1266808; AID1415637; AID1622954 |
| Histone deacetylase 9 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0005 | 0.9413 | 9.9000 | AID1266808; AID1415637; AID1622954 |
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | GI50 | 1.6700 | 0.2790 | 1.1052 | 1.9500 | AID1635791; AID1635792; AID1635793 |
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | IC50 (µMol) | 5.0800 | 0.0040 | 1.9666 | 10.0000 | AID1635783 |
| Histone deacetylase 5 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0007 | 0.9610 | 10.0000 | AID1266808; AID1415637; AID1622954 |
| Transporter | Rattus norvegicus (Norway rat) | Ki | 3.2600 | 0.0001 | 0.8667 | 10.0000 | AID145367 |
| Nischarin | Homo sapiens (human) | Ki | 6.9110 | 0.0042 | 0.2192 | 3.8019 | AID223227; AID223242 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1B | Homo sapiens (human) | IC50 (µMol) | 0.1183 | 0.0010 | 0.5851 | 4.4200 | AID1203149; AID1284863; AID1441345; AID1714122; AID707508 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1B | Homo sapiens (human) | Ki | 0.1660 | 0.1660 | 0.1660 | 0.1660 | AID752776 |
| [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) |
|---|---|---|---|---|---|---|---|
| CDC-like kinase 1, isoform CRA_c | Homo sapiens (human) | AC50 | 0.0173 | 0.0019 | 2.2088 | 16.9100 | AID588811 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1347363 | Firefly luciferase counterscreen qHTS: Assay Interference Panel against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347368 | G06 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347387 | Cytotoxicity qHTS for assessment of Hepg2 cells membrane integrity screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347373 | qHTS for Constitutive Androstane Receptor (CAR) Agonist screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347402 | qHTS for inhibitors of Rabies Virus screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347380 | qHTS for Antimalaria activity screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347391 | qHTS for activators of Nrf2/ARE signaling pathway screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347346 | HPAF-II Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347350 | SW1088 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347381 | Inflammasome Signaling qHTS Counterscreen: IL-1-beta AlphaLISA counterscreen against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347359 | HEK293 24hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347356 | HPAF-II 24hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| 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. |
| AID1347377 | DH5-alpha competent E. coli microbial cell viability qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347394 | Vero-766 cells viability qHTS against the NCATS CANVASS Library: Counterscreen for Zika virus inhibition assay | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347360 | HPAF-II 18hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347371 | J3T Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347401 | Redox Reaction Profiling qHTS: Assay Interference Panel against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347365 | SDT Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347351 | U-118MG Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347396 | qHTS for inhibitors of Wild type Zika virus screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347369 | MCF7 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347400 | Viability qHTS for inhibitors of the SERCaMP assay screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347347 | UWB1.289 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347345 | OV-KATE Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347353 | A2780 Cisplatin Sensitive Ovarian Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347389 | qHTS assay for small molecule disruptors of mitochondrial membrane potential screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347375 | qHTS for Hypoxia signaling pathway (HIF-1) agonists against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347393 | qHTS for inhibitors of ER calcium dysfunction: SERCaMP assay screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347349 | Panc-1005 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347374 | qHTS for Hypoxia signaling pathway (HIF-1) antagonists against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347358 | HPAF-II 12hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347372 | qHTS for Constitutive Androstane Receptor (CAR) Antagonist screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347348 | OV-SAHO Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347366 | KB-3-1 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347354 | UWB1.289-WTBRCA1 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347390 | Secretion counterscreen for inhibitors of the SERCaMP assay screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347352 | COV-362 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347370 | qHTS for ATAD5 Antagonist screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347364 | KB-8-5-11 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347376 | 10-beta competent E. coli microbial cell viability qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347357 | HEK293 18hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347362 | Diaphorse counterscreen qHTS: Assay Interference Panel against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347361 | HEK293 12hr Apoptosis Induction qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347388 | qHTS for Activators of p53 Stress Response Pathway screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347392 | qHTS for activators of dead-cell proteases activity screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347379 | qHTS for Inflammasome Signaling Inhibitors: IL-1-beta AlphaLISA screen against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347355 | HEK-293 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347367 | qHTS for ATAD5 Agonist screened against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1347378 | qHTS for H2AX Agonists against the NCATS CANVASS Library | 2018 | ACS central science, Dec-26, Volume: 4, Issue:12 | Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. |
| AID1859908 | Selectivity index, ratio of IC50 for cytotoxicity against human HepG2 cells to IC50 for antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents. |
| AID1417152 | Binding affinity to full length wild type human DYRK2 (M1 to S528 residues) expressed in mammalian expression system assessed as remaining unbound target protein level at 10 uM by Kinomescan method relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel selective thiadiazine DYRK1A inhibitor lead scaffold with human pancreatic β-cell proliferation activity. |
| AID653129 | Inhibition of DYRK2 | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5 | Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors. |
| AID1859900 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite growth incubated for 3 days by HRP2-ELISA | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents. |
| AID1181723 | Antimicrobial activity against trypamastigote stage of Trypanosoma brucei after 72 hrs by Alamar Blue assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Synthesis, antileishmanial and antitrypanosomal activities of N-substituted tetrahydro-β-carbolines. |
| AID1356561 | Inhibition of human DAPK2 expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID63034 | Binding affinity towards Dopamine receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID1356555 | Inhibition of human CSNK1D expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID6517 | Binding affinity towards human 5-hydroxytryptamine 6 receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID1762309 | Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Bioinspired imidazo[1,2-a:4,5-c']dipyridines with dual antiproliferative and anti-migrative properties in human cancer cells: The SAR investigation. |
| AID1543930 | Antiproliferative activity against human SMMC7721 cells incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
| AID1356578 | Inhibition of human TGFBR2 expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1823511 | Inhibition of CDK11 (unknown origin) in human CAL-27 cells measured after 6 hrs by select screen kinase assay | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID724338 | Cytotoxicity against human A549 cells by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID752776 | Competitive inhibition of GST-tagged DYRK1B (unknown origin) expressed in Escherichia coli BL21(DE3) by Lineweaver-Burk plot analysis in presence of ATP | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12 | Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315. |
| AID1356550 | Inhibition of human CIT expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID724341 | Cytotoxicity against human HepG2 cells by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID1403159 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
| AID1578908 | Induction of autophagy in human Bel7402 cells assessed as accumulation of autophagic vacuoles at 20 uM after 24 hrs by acridine orange staining based fluorescence microscopic method | 2019 | Journal of natural products, 06-28, Volume: 82, Issue:6 | Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways. |
| AID1165916 | Inhibition of GSK3alpha/beta (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21 | Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors. |
| AID1478836 | Inhibition of full-length recombinant human GST-tagged Dyrk1a expressed in baculovirus expression system using Alexa-Fluor tracer-236 incubated for 60 mins by TR-FRET based Lantha-screen Eu kinase assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Developing DYRK inhibitors derived from the meridianins as a means of increasing levels of NFAT in the nucleus. |
| AID707482 | Binding affinity to CLK1 | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID435867 | Percentage NEK2a activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID673516 | Antiproliferative activity against human COLO205 cells by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15 | InCl3-catalysed synthesis of 2-aryl quinazolin-4(3H)-ones and 5-aryl pyrazolo[4,3-d]pyrimidin-7(6H)-ones and their evaluation as potential anticancer agents. |
| AID1493937 | Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis and biological evaluation of new β-carboline-bisindole compounds as DNA binding, photocleavage agents and topoisomerase I inhibitors. |
| AID1356547 | Inhibition of human CDK7 expressed in mammalian expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID435260 | Percentage RSK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID722897 | Antitumor activity in mouse CT26 colon cancer cells inoculated mouse assessed as tumor inhibition rate at one fifth of LD50 concentration once a day for consecutive 7 days by ip | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Design, synthesis and in vitro and in vivo antitumor activities of novel bivalent β-carbolines. |
| AID53689 | Inhibition of Cyclin-dependent kinase 2-cyclin A | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | Beta-carbolines as specific inhibitors of cyclin-dependent kinases. |
| AID1752367 | Antiproliferative activity against human EML4-ALK positive H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Harmine-inspired design and synthesis of benzo[d]imidazo[2,1-b]thiazole derivatives bearing 1,3,4-oxadiazole moiety as potential tumor suppressors. |
| AID357032 | Cytotoxicity against human H9 cells | 2001 | Journal of natural products, Jul, Volume: 64, Issue:7 | Anti-AIDS agents. 46. Anti-HIV activity of harman, an anti-HIV principle from Symplocos setchuensis, and its derivatives. |
| AID1752369 | Inhibition of epithelial-mesenchymal transition in human A549 cells assessed as suppression of Twist 1 expression at 17 uM measured after 24 hrs by Western blot analysis | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Harmine-inspired design and synthesis of benzo[d]imidazo[2,1-b]thiazole derivatives bearing 1,3,4-oxadiazole moiety as potential tumor suppressors. |
| AID435378 | Percentage S6K1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1420021 | Inhibition of human recombinant full length GST-tagged DYRK1A expressed in baculovirus expression system assessed as decrease in tau phosphorylation at S396 preincubated for 10 mins followed by tau addition by Western blot analysis | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics. |
| AID108345 | Binding affinity towards Glutamate (rPCP) receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID491358 | Inhibition of pig brain topoisomerase 2-mediated supercoiled DNA relaxation after 20 mins by agarose gel electrophoresis analysis | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Kinesin spindle protein (KSP) inhibitors with 2,3-fused indole scaffolds. |
| AID1665558 | Antiproliferative activity against rat 9L-2 cells by MTT assay | |||
| AID94188 | In vitro cytotoxic activity was determined against drug resistant tumor cell line KB-CPT (pleotrophic mechanism including level of topoisomerase I) | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Antitumor agents 201. Cytotoxicity of harmine and beta-carboline analogs. |
| AID1627155 | Cytotoxicity against human SGC7901 cells assessed as inhibition of cell growth after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Synthesis and biological evaluation of N(9)-substituted harmine derivatives as potential anticancer agents. |
| AID37207 | Binding affinity towards Alpha-1B adrenergic receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID201791 | In vitro cytotoxic activity was determined against melanoma cancer (SK-MEL-2) cell line | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Antitumor agents 201. Cytotoxicity of harmine and beta-carboline analogs. |
| AID1823492 | Induction of apoptosis in human CAL-27 cells assessed as decrease in FOXO3A phosphorylation at serine 253 residue at 5 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1165914 | Inhibition of DYRK1A (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21 | Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors. |
| AID1547013 | Binding affinity to wild-type human partial length HASPIN (I452 to K798 residues) expressed in mammalian expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID724343 | Cytotoxicity against human BGC823 cells by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID417454 | Cytotoxicity against human HepG2 cells by MTT assay | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis and in vitro cytotoxic evaluation of novel 3,4,5-trimethoxyphenyl substituted beta-carboline derivatives. |
| AID40566 | Binding affinity towards Beta-1A adrenergic receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID1493938 | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis and biological evaluation of new β-carboline-bisindole compounds as DNA binding, photocleavage agents and topoisomerase I inhibitors. |
| AID1665559 | Cytotoxicity against human CCD-841 cells by MTT assay | |||
| AID55536 | Percentage inhibition against cyclin dependent kinase 5 (CDK 5) at a concentration of 50 uM | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | Beta-carbolines as specific inhibitors of cyclin-dependent kinases. |
| AID39935 | Binding affinity towards GABA-A benzodiazepine receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID165278 | Inhibition of protein kinase C | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | Beta-carbolines as specific inhibitors of cyclin-dependent kinases. |
| AID1769948 | Cytotoxicity against human HepG2 cells assessed as cell growth inhibition incubated for 1 day by neutral red assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Further investigation of harmicines as novel antiplasmodial agents: Synthesis, structure-activity relationship and insight into the mechanism of action. |
| AID1547014 | Binding affinity to wild-type human partial length HIPK2 (M153 to S564 residues) expressed in mammalian expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1105364 | Herbicidal activity against Brassica rapa subsp. oleifera assessed as growth inhibition at 10 ug/ml | 2012 | Molecules (Basel, Switzerland), Apr-02, Volume: 17, Issue:4 | Synthesis and herbicidal activity evaluation of novel β-carboline derivatives. |
| AID1356571 | Inhibition of human IRAK1 expressed in mammalian expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1543968 | Induction of DNA damage in human Bel7402/5-FU cells assessed as increase in phosphorylated H2AX levels at 20 uM incubated for 72 hrs by Western blot assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
| AID436036 | Percentage Lck activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID707483 | Binding affinity to DYRK2 | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1266811 | Antiproliferative activity against human SW620 cells assessed as cell viability after 48 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway. |
| AID435734 | Percentage NEK6 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1765304 | Improvement in learning and spatial memory in mouse harboring APP/PSI/Tau assessed as improvement in trajectory at 20 mg/kg, po for 30 consecutive days and studied for 5 days by Morris water maze test relative to control | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease. |
| AID435461 | Percentage CK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID479486 | Displacement of bis-ANS from human Hsp90 assessed as reduction in fluorescence at 100 uM after 30 mins by fluorescent monochromator spectrophotometry | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | A repurposing strategy identifies novel synergistic inhibitors of Plasmodium falciparum heat shock protein 90. |
| AID1545908 | Antiproliferative activity against human HGC27 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
| AID721729 | Inhibition of DYRK3 (unknown origin) | 2013 | European journal of medicinal chemistry, Jan, Volume: 59 | Synthesis and biological evaluation of N-aryl-7-methoxybenzo[b]furo[3,2-d]pyrimidin-4-amines and their N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amine analogues as dual inhibitors of CLK1 and DYRK1A kinases. |
| AID1762326 | Antimigratory activity in human MDA-MB-435 cells assessed as inhibition of cell migration at 1 uM after 24 hrs by wound healing assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Bioinspired imidazo[1,2-a:4,5-c']dipyridines with dual antiproliferative and anti-migrative properties in human cancer cells: The SAR investigation. |
| AID1467084 | Inhibition of recombinant human CDK2/cyclin A using histone H1 as substrate after 30 mins in presence of ATP by scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | N-(1H-Pyrazol-3-yl)quinazolin-4-amines as a novel class of casein kinase 1δ/ε inhibitors: Synthesis, biological evaluation and molecular modeling studies. |
| AID707498 | Inhibition of Leishmania major recombinant CK1 expressed in Escherichia coli using RRKHAAIGpSAYSITA as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID656680 | Inhibition of electric eel AChE using acetylcholine iodide as substrate measured every 5 sec for 2 mins by Ellman's method | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Prospective acetylcholinesterase inhibitory activity of indole and its analogs. |
| AID721734 | Inhibition of porcine brain CK1delta/epsilon using RRKHAAIGpSAYSITA as substrate | 2013 | European journal of medicinal chemistry, Jan, Volume: 59 | Synthesis and biological evaluation of N-aryl-7-methoxybenzo[b]furo[3,2-d]pyrimidin-4-amines and their N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amine analogues as dual inhibitors of CLK1 and DYRK1A kinases. |
| AID1356546 | Inhibition of human CDK11 expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID6482 | Binding affinity towards 5-HT5A receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID435854 | Percentage IKK-beta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435374 | Percentage PLK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1356564 | Inhibition of human DYRK1A expressed in mammalian expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID724319 | Antitumor activity against mouse Sarcoma 180 cells xenografted in mouse assessed as tumor inhibition at 7.5 mg/kg, ip qd for 7 days measured every 3 days for 21 days | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID1547008 | Binding affinity to wild-type human full length CSNK1G2 (M1 to K415 residues) expressed in bacterial expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID103712 | In vitro cytotoxic activity against MCF-7 (human breast cancer) cell line. | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Antitumor agents 201. Cytotoxicity of harmine and beta-carboline analogs. |
| AID5615 | Binding affinity towards 5-hydroxytryptamine 2C receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID977602 | Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID1226068 | Drug level in late stage L4 Caenorhabditis elegans treated with 2-(Cyclopropylmethyl)-7-methoxy-1-methyl-9H-pyrido[3,4-b]indol-2-ium bromide at 10 uM after 6 hrs by LC-MS analysis | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Exploiting the Polypharmacology of ß-Carbolines to Disrupt O. volvulus Molting. |
| AID721735 | Inhibition of porcine brain GSK3alpha/beta using GS-1 as substrate | 2013 | European journal of medicinal chemistry, Jan, Volume: 59 | Synthesis and biological evaluation of N-aryl-7-methoxybenzo[b]furo[3,2-d]pyrimidin-4-amines and their N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amine analogues as dual inhibitors of CLK1 and DYRK1A kinases. |
| AID722893 | Antitumor activity in mouse H22 liver cancer cells inoculated mouse assessed as tumor inhibition rate at one fifth of LD50 concentration once a day for consecutive 7 days by ip | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Design, synthesis and in vitro and in vivo antitumor activities of novel bivalent β-carbolines. |
| AID94014 | In vitro cytotoxic activity was determined against drug resistant tumor cell line KB-7d (pleotrophic resistance including MRP multidrug resistant protein) | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Antitumor agents 201. Cytotoxicity of harmine and beta-carboline analogs. |
| AID1546962 | Inhibition of DYRK1A in mouse R7T1 cells expressing expressing NFAT2-GFP assessed as induction of NFAT2- GFP nuclear translocation at 10 uM incubated for 24 hrs | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1266808 | Inhibition of HDAC in human HeLa cell nuclear extract using Boc-Lys (Ac)-AMC as substrate after 60 mins by fluorometric analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway. |
| AID435723 | Percentage GSK3-beta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1545852 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
| AID1356537 | Inhibition of GST-tagged human recombinant DYRK1A by FRET-based LanthaScreen Eu kinase binding assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1091983 | Cytotoxicity against Spodoptera frugiperda (fall armyworm) Sf9 cells assessed as growth inhibition at 200 mg/L after 24 hr by MTT assay | 2010 | Molecules (Basel, Switzerland), Nov-02, Volume: 15, Issue:11 | Cytotoxic and insecticidal activities of derivatives of harmine, a natural insecticidal component isolated from Peganum harmala. |
| AID1266813 | Antiproliferative activity against human SW480 cells assessed as cell viability after 48 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway. |
| AID1356558 | Inhibition of human CSNK2A1 expressed in mammalian expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1543933 | Antiproliferative activity against human H1299 cells incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
| AID724344 | Cytotoxicity against human HeLa cells by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID1851169 | Inhibition of MAOA (unknown origin) | 2022 | Bioorganic & medicinal chemistry, 09-15, Volume: 70 | A critical update on the strategies towards small molecule inhibitors targeting Serine/arginine-rich (SR) proteins and Serine/arginine-rich proteins related kinases in alternative splicing. |
| AID1543931 | Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
| AID1890953 | Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 65 | Synthesis of harmine-nitric oxide donor derivatives as potential antitumor agents. |
| AID697219 | Solubility of compound at pH 7.4 | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | Novel trisubstituted harmine derivatives with original in vitro anticancer activity. |
| AID697233 | Growth inhibition of human U373 cells after 3 days by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | Novel trisubstituted harmine derivatives with original in vitro anticancer activity. |
| AID435570 | Inhibition of DYRK1A in the presence of 50uM ATP | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1581639 | Selectivity index, ratio of IC50 for human HepG2 cells to IC50 for Plasmodium falciparum 3D7 | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Harmicines - harmine and cinnamic acid hybrids as novel antiplasmodial hits. |
| AID1578884 | Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay | 2019 | Journal of natural products, 06-28, Volume: 82, Issue:6 | Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways. |
| AID436037 | Percentage MAPKAPK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1546995 | Ratio of drug level in CD1 mouse brain to plasma at 30 mg/kg, ip | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID233027 | Relative activity against FM3A cells and Plasmodium falciparum FCR3 | 2004 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 14, Issue:7 | Pi-delocalized beta-carbolinium cations as potential antimalarials. |
| AID724342 | Cytotoxicity against human Bel7402 cells by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID82702 | In vitro cytotoxic activity was determined against embryonic lung fibroblast (HEL) cell line | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Antitumor agents 201. Cytotoxicity of harmine and beta-carboline analogs. |
| AID1284862 | Inhibition of recombinant human N-terminal His6-tagged DYRK1A catalytic domain expressed in Escherichia coli BL21(DE3) cells using KKISGRLSPIMTEQ-NH2 as substrate incubated for 15 mins in presence of [gamma-32P]ATP | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2. |
| AID1226061 | Inhibition of Brugia malayi chitinase using 4-methylumbelliferyl-N-N'-N''-beta-chitotrioside as substrate assessed as release of 4-methylumbelliferone at 10 uM measured for 10 mins by fluorescence assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Exploiting the Polypharmacology of ß-Carbolines to Disrupt O. volvulus Molting. |
| AID473138 | Antiplatelet aggregation activity against collagen-induced platelet | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | A class of 3S-2-aminoacyltetrahydro-beta-carboline-3-carboxylic acids: their facile synthesis, inhibition for platelet activation, and high in vivo anti-thrombotic potency. |
| AID94194 | In vitro cytotoxic activity was determined against drug resistant tumor cell line KB-VIN (expressing P-glycoprotein) | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Antitumor agents 201. Cytotoxicity of harmine and beta-carboline analogs. |
| AID1181719 | Antimicrobial activity against bloodstream form of Trypanosoma brucei brucei TC221 | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Synthesis, antileishmanial and antitrypanosomal activities of N-substituted tetrahydro-β-carbolines. |
| AID1356554 | Inhibition of human CSNK1A1 expressed in mammalian expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1547012 | Binding affinity to wild-type human full length DYRK2 (M1 to S528 residues) expressed in mammalian expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1665556 | Antiproliferative activity against human HT-29 cells by MTT assay | |||
| AID1356557 | Inhibition of human CSNK1G2 expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID435338 | Percentage CaMK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435577 | Inhibition of PIM3 in the presence of 20uM ATP | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1203150 | Inhibition of GST-tagged Dyrk2 (unknown origin) expressed in Escherichia coli using [33P]ATP[gammaP]/DYRKtide as substrate after 5 mins by liquid scintillation counting analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis. |
| AID724129 | Antitumor activity against mouse LLC cells xenografted in mouse assessed as tumor inhibition at 7.5 mg/kg, ip qd for 7 days measured every 3 days for 21 days | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID1546963 | Induction of beta-cell proliferation in rat pancreatic islets at 10 uM incubated for 96 hrs by Ki67-insulin co-immunolabeling assay | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1545858 | Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
| AID724333 | Cytotoxicity against human 769-P cells by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID1546980 | Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in CHOK1 cells at 10 uM incubated for 60 mins by radiometric enzymatic assay relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1356985 | Inhibition of human DYRK1A expressed in HEK293 cells assessed as inhibition of NFAT transcriptional activity at 5 uM by NFAT response element-driven luciferase reporter gene assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors. |
| AID417455 | Cytotoxicity against human MCF7 cells by MTT assay | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis and in vitro cytotoxic evaluation of novel 3,4,5-trimethoxyphenyl substituted beta-carboline derivatives. |
| AID1284867 | Inhibition of EGFR (unknown origin) incubated for 15 mins in presence of [gamma-32P]ATP | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2. |
| AID1478837 | Inhibition of full-length recombinant human His-tagged GSK3B recombinant in baculovirus expression system using Alexa-Fluor tracer-236 incubated for 60 mins by TR-FRET based Lantha-screen Eu kinase assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Developing DYRK inhibitors derived from the meridianins as a means of increasing levels of NFAT in the nucleus. |
| AID1181717 | Antimicrobial activity against promastigote stage of Leishmania infantum | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Synthesis, antileishmanial and antitrypanosomal activities of N-substituted tetrahydro-β-carbolines. |
| AID1356563 | Inhibition of human DRAK2 expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID343385 | Inhibition of Trypanosoma cruzi recombinant trypanothione reductase at 85 uM | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | The use of natural product scaffolds as leads in the search for trypanothione reductase inhibitors. |
| AID1091980 | Insecticidal activity against fourth-instar larval stage of Culex quinquefasciatus assessed as increase in mortality at 50 to 100 mg/L after 24 hr | 2010 | Molecules (Basel, Switzerland), Nov-02, Volume: 15, Issue:11 | Cytotoxic and insecticidal activities of derivatives of harmine, a natural insecticidal component isolated from Peganum harmala. |
| AID1356574 | Inhibition of human PIM1 expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID357033 | Antiviral activity against HIV1 in human H9 cells assessed as inhibition of viral replication | 2001 | Journal of natural products, Jul, Volume: 64, Issue:7 | Anti-AIDS agents. 46. Anti-HIV activity of harman, an anti-HIV principle from Symplocos setchuensis, and its derivatives. |
| AID1546996 | Induction of pancreatic beta-cells proliferation in C57BL6N mouse assessed as increase in beta-cell Ki67 immuno-labeling dosed daily via intraperitoneal route for 7 days | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID223227 | Binding affinity towards Imidazoline I1 receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID1900714 | Inhibition of GSK3-beta (unknown origin) incubated for 60 mins by ATP-Glo luminescent assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease. |
| AID453494 | Inhibition of human MAOA | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2 | Proposed structural basis of interaction of piperine and related compounds with monoamine oxidases. |
| AID479487 | Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes after 48 hrs by flow-cytometry | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | A repurposing strategy identifies novel synergistic inhibitors of Plasmodium falciparum heat shock protein 90. |
| AID707255 | Binding affinity to casein kinase 1 | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID656681 | Inhibition of electric eel AChE using acetylcholine iodide as substrate at 10'-4 M measured every 5 sec for 2 mins by Ellman's method | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Prospective acetylcholinesterase inhibitory activity of indole and its analogs. |
| AID1890984 | Acute toxicity in ICR mouse assessed as death time at 10 mg/kg, ip measured over 14 days | 2022 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 65 | Synthesis of harmine-nitric oxide donor derivatives as potential antitumor agents. |
| AID1547015 | Binding affinity to wild-type human partial length HIPK3 (M153 to N562 residues) expressed in mammalian expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1823491 | Induction of apoptosis in human CAL-27 cells assessed as decrease in FOXO3A phosphorylation at serine 253 residue at 1 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1356562 | Inhibition of human DAPK3 expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1547007 | Binding affinity to wild-type human full length CSNK1E (M1 to K416 residues) expressed in bacterial expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1581636 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 erythrocytic stage measured after 3 days by HRP2 assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Harmicines - harmine and cinnamic acid hybrids as novel antiplasmodial hits. |
| AID435373 | Percentage PKCzeta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1330649 | Inhibition of CLK1 (unknown origin) | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis, biological evaluation and molecular modeling studies of imidazo[1,2-a]pyridines derivatives as protein kinase inhibitors. |
| AID1105363 | Herbicidal activity against Echinochloa crus-galli (barnyard grass) assessed as growth inhibition at 100 ug/ml | 2012 | Molecules (Basel, Switzerland), Apr-02, Volume: 17, Issue:4 | Synthesis and herbicidal activity evaluation of novel β-carboline derivatives. |
| AID1543929 | Inhibition of HDAC1 (unknown origin) using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins and measured after 30 mins by fluorescence assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
| AID1356535 | Inhibition of GST-tagged human recombinant DYRK1A at 1000 nM by FRET-based LanthaScreen Eu kinase binding assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1420030 | Inhibition of GST-tagged DYRK1A (unknown origin) expressed in Escherichia coli DH5alpha at 1 uM using RRRFRPASPLRGPPK as substrate after 30 mins by kinase-glo luminescence assay relative to control | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics. |
| AID1635791 | Reversal of human ABCG2-mediated resistance to SN-38 in human ABCG2 expressed MDCK2 cells assessed as SN-38 GI50 at 0.01 uM after 72 hrs by MTT assay (Rvb SN-38 alone GI50 = 2.28 +/- 0.39 uM) | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Synthesis and Investigation of Tetrahydro-β-carboline Derivatives as Inhibitors of the Breast Cancer Resistance Protein (ABCG2). |
| AID1335819 | Inhibition of human recombinant CDK5/p25 using histone H1 as substrate after 30 mins in presence of [gamma-33 P] ATP by liquid scintillation counting analysis | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors. |
| AID1546978 | Displacement of [3H]rauwoiscine from human recombinant adrenergic alpha2B receptor expressed in CHOK1 cells at 10 uM incubated for 60 mins by radiometric enzymatic assay relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID724330 | Cytotoxicity against human 22Rv1 cells by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID1714121 | Inhibition of human DYRK1A using [33P]-ATP incubated for 120 mins | 2016 | Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22 | An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases. |
| AID1546958 | Inhibition of DYRK1A (unknown origin) by FRET-based Lantha-screen Eu kinase binding assay | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID707505 | Inhibition of human recombinant GST-tagged DYRK4 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1403160 | Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
| AID1543955 | Induction of apoptosis in human Bel7402/5-FU cells assessed as late apoptotic cells at 20 uM incubated for 72 hrs by FITC-Annexin V/PI staining based flow cytometry (Rvb = 1.01%) | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
| AID1823510 | Inhibition of CDK8 (unknown origin) in human CAL-27 cells measured after 6 hrs by select screen kinase assay | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1823490 | Induction of apoptosis in human CAL-27 cells assessed as decrease in FOXO3A phosphorylation at serine 253 residue at 0.5 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1356577 | Inhibition of human RPS6KA4 (Kin.Dom.2-C-terminal) expressed in mammalian expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1432638 | Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability after 24 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6 | Synthesis of novel spiro[pyrazolo[4,3-d]pyrimidinones and spiro[benzo[4,5]thieno[2,3-d]pyrimidine-2,3'-indoline]-2',4(3H)-diones and their evaluation for anticancer activity. |
| AID435747 | Percentage PRAK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID95653 | In vitro cytotoxic activity was determined against epidermoid carcinoma of the nasopharynx (KB) cell line | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Antitumor agents 201. Cytotoxicity of harmine and beta-carboline analogs. |
| AID435706 | Percentage BRSK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1432636 | Cytotoxicity against human K562 cells assessed as decrease in cell viability after 24 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6 | Synthesis of novel spiro[pyrazolo[4,3-d]pyrimidinones and spiro[benzo[4,5]thieno[2,3-d]pyrimidine-2,3'-indoline]-2',4(3H)-diones and their evaluation for anticancer activity. |
| AID1859903 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 assessed as inhibition of parasite growth incubated for 3 days by HRP2-ELISA | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents. |
| AID435370 | Percentage p38beta MAPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435427 | Percentage PKBalpha activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435539 | Percentage PHK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID722908 | Cytotoxicity against human ovary adenocarcinoma SKOV3 cells assessed as reduction in optical density by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Design, synthesis and in vitro and in vivo antitumor activities of novel bivalent β-carbolines. |
| AID707683 | Inhibition of human recombinant full length GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID357034 | Therapeutic index, ratio of IC50 for human H9 cells to EC50 for HIV1 | 2001 | Journal of natural products, Jul, Volume: 64, Issue:7 | Anti-AIDS agents. 46. Anti-HIV activity of harman, an anti-HIV principle from Symplocos setchuensis, and its derivatives. |
| AID145367 | Binding affinity towards NET | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID435493 | Percentage PKD1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID491357 | Inhibition of pig brain topoisomerase 1-mediated supercoiled DNA relaxation after 20 mins by agarose gel electrophoresis analysis | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Kinesin spindle protein (KSP) inhibitors with 2,3-fused indole scaffolds. |
| AID1547003 | Binding affinity to wild-type human partial length CLK2 (D144 to R498 residues) expressed in bacterial expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1635792 | Reversal of human ABCG2-mediated resistance to SN-38 in human ABCG2 expressed MDCK2 cells assessed as SN-38 GI50 at 0.1 uM after 72 hrs by MTT assay (Rvb SN-38 alone GI50 = 2.28 +/- 0.39 uM) | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Synthesis and Investigation of Tetrahydro-β-carboline Derivatives as Inhibitors of the Breast Cancer Resistance Protein (ABCG2). |
| AID1091975 | Insecticidal activity against Lipaphis erysimi (mustard aphids) assessed as mortality at 200 mg/L after 48 hr | 2010 | Molecules (Basel, Switzerland), Nov-02, Volume: 15, Issue:11 | Cytotoxic and insecticidal activities of derivatives of harmine, a natural insecticidal component isolated from Peganum harmala. |
| AID1441346 | Inhibition of full-length recombinant human GST-tagged DYRK4 expressed in baculovirus infected insect cells using DYRKtide as substrate after 5 mins in presence of [gamma-33P]ATP by liquid scintillation counting | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Structural Optimization and Pharmacological Evaluation of Inhibitors Targeting Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases (DYRK) and CDC-like kinases (CLK) in Glioblastoma. |
| AID1546999 | Induction of pancreatic beta-cells proliferation in immunodeficient NOD-SCID mouse with human islets transplanted into renal capsule at 10 mg/kg, ip dosed daily for 7 days relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1415639 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
| AID1765288 | Inhibition of human recombinant full length GSK3beta expressed in baculovirus in Sf9 insect cells using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate at 10 uM by ADP-Glo kinase assay relative to control | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease. |
| AID1356570 | Inhibition of human HIPK3 expressed in mammalian expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1356553 | Inhibition of human CLK4 expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1330648 | Inhibition of DYRK1A (unknown origin) | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis, biological evaluation and molecular modeling studies of imidazo[1,2-a]pyridines derivatives as protein kinase inhibitors. |
| AID1900709 | Inhibition of equine serum BChE at 50 uM using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease. |
| AID1713264 | Antileishmanial activity against late log phase promastigote stage of Leishmania infantum MHOM/FR/78/LEM75 assessed as inhibition of parasite growth incubated for 48 hrs by hemocytometer counting method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and anti-leishmanial evaluation of 1-phenyl-2,3,4,9-tetrahydro-1H-β-carboline derivatives against Leishmania infantum. |
| AID1900712 | Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease. |
| AID707507 | Inhibition of human recombinant GST-tagged DYRK2 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1752366 | Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Harmine-inspired design and synthesis of benzo[d]imidazo[2,1-b]thiazole derivatives bearing 1,3,4-oxadiazole moiety as potential tumor suppressors. |
| AID1890949 | Antiproliferative activity against human BGC-823 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 65 | Synthesis of harmine-nitric oxide donor derivatives as potential antitumor agents. |
| AID435300 | Percentage PAK6 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1546982 | Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells at 10 uM incubated for 2 hrs by radiometric enzymatic assay relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID223253 | Binding affinity at rat imidazoline receptor I-2 | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4 | Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation. |
| AID1896381 | Inhibition of recombinant human MAO-A using using kynuramine as substrate assessed as inhibition of 4-hydroxyquinoline formation incubated for 20 mins by fluorescence spectrophotometric analysis | 2022 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 77 | The inhibition of monoamine oxidase by 2H-1,4-benzothiazin-3(4H)-ones. |
| AID1665606 | Induction of autophagy in human HT-29 cells assessed as reduction in p62 protein level at 10 uM incubated for 72 hrs by Western blot analysis | |||
| AID707477 | Binding affinity to CLK2 | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1356556 | Inhibition of human CSNK1E expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID435123 | Percentage NEK7 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1665597 | Induction of apoptosis in human HT-29 cells assessed as increase in cleaved PARP protein level at 10 uM incubated for 72 hrs by Western blot analysis | |||
| AID1441344 | Inhibition of full-length recombinant human GST-tagged DYRK3 expressed in Escherichia coli using woodtide as substrate after 30 mins in presence of [gamma-33P]ATP | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Structural Optimization and Pharmacological Evaluation of Inhibitors Targeting Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases (DYRK) and CDC-like kinases (CLK) in Glioblastoma. |
| AID2964 | In vitro cytotoxic activity was determined against ovarian cancer (1A9) cell line | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Antitumor agents 201. Cytotoxicity of harmine and beta-carboline analogs. |
| AID1543973 | Induction of autophagy in human Bel7402/5-FU cells assessed as up regulation of LC3-2 levels at 20 uM incubated for 72 hrs by Western blot assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
| AID1356567 | Inhibition of human HASPIN expressed in mammalian expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID656685 | Inhibition of human AChE at 10'-4 M by Ellman's method | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Prospective acetylcholinesterase inhibitory activity of indole and its analogs. |
| AID1356568 | Inhibition of human HIPK1 expressed in mammalian expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1284866 | Inhibition of recombinant human GST-tagged CLK1 catalytic domain (129 to 484 residues) expressed in Escherichia coli using GRSRSRSRSRSRSRSR as substrate incubated for 15 mins in presence of [gamma-32P]ATP | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2. |
| AID6591 | Binding affinity towards 5-hydroxytryptamine 7 receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID1823461 | Induction of apoptosis in human CAL-27 cells assessed as increase in cleaved-PARP level at 10 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1823480 | Antiproliferative activity against human HEK293T cells assessed as reduction in cell viability at 10 uM measured after 72 hrs by Celltiter-Glo luminescent assay | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1900710 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease. |
| AID1546984 | Displacement of [125I]RTI55 from human recombinant NET expressed in CHOK1 cells at 10 uM incubated for 2 hrs by radiometric enzymatic assay relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1578899 | Induction of apoptosis in human Bel7402 cells assessed as annexin-V positive cells at 20 uM after 72 hrs by Annexin-V/PI staining based flow cytometry relative to control | 2019 | Journal of natural products, 06-28, Volume: 82, Issue:6 | Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways. |
| AID1105365 | Herbicidal activity against Brassica rapa subsp. oleifera assessed as growth inhibition at 100 ug/ml | 2012 | Molecules (Basel, Switzerland), Apr-02, Volume: 17, Issue:4 | Synthesis and herbicidal activity evaluation of novel β-carboline derivatives. |
| AID1546985 | Toxicity in C57BL6N mouse assessed as induction of tremor at rest and during movement lasting 5 to 15 mins at 10 mg/kg, ip | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1441342 | Inhibition of recombinant human GST-tagged DYRK1A (1 to 499 amino acid residues) expressed in Escherichia coli using woodtide as substrate after 30 mins in presence of [gamma-33P]ATP | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Structural Optimization and Pharmacological Evaluation of Inhibitors Targeting Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases (DYRK) and CDC-like kinases (CLK) in Glioblastoma. |
| AID1420026 | Inhibition of human full length DYRK1A using KKISGRLSPIMTEQ as substrate after 30 mins in presence of [gamma33P-ATP] | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics. |
| AID636105 | Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Ultrasound mediated catalyst free synthesis of 6H-1-benzopyrano[4,3-b]quinolin-6-ones leading to novel quinoline derivatives: their evaluation as potential anti-cancer agents. |
| AID479489 | Antimalarial activity against multidrug-resistant Plasmodium falciparum isolate 208432 infected in human erythrocytes after 48 hrs by flow-cytometry | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | A repurposing strategy identifies novel synergistic inhibitors of Plasmodium falciparum heat shock protein 90. |
| AID707504 | Inhibition of rat recombinant ERK2 using Ets1 as substrate and [gamma33P]ATP as substrate after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1769946 | Antiplasmodial activity against chloroquine-resistant erythrocytic stage Plasmodium falciparum Dd2 assessed as inhibition of parasite growth incubated for 3 days by HRP2-ELISA | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Further investigation of harmicines as novel antiplasmodial agents: Synthesis, structure-activity relationship and insight into the mechanism of action. |
| AID435315 | Percentage MARK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID707693 | Inhibition of human recombinant CDK7/cyclin H expressed in insect cell using YSPTSPSYSPTSPSYSPTSPSKKKK as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1356552 | Inhibition of human CLK2 expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID126913 | Inhibition of Mitogen-activated protein kinase | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | Beta-carbolines as specific inhibitors of cyclin-dependent kinases. |
| AID4616 | Binding affinity towards 5-hydroxytryptamine 1D receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID1546955 | Toxicity in C57BL6N mouse assessed as induction of tremor lasting 5 to 15 mins at 10 mg/kg, ip | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1335828 | Inhibition of recombinant human DYRK1A (1 to 499 residues) expressed in Escherichia coli using woodtide as substrate incubated for 30 mins in presence of [gamma-33 P] ATP by liquid scintillation counting analysis | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors. |
| AID707476 | Binding affinity to DYRK1B | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1588124 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15 | Synthesis and in vitro cytotoxicity evaluation of β-carboline-combretastatin carboxamides as apoptosis inducing agents: DNA intercalation and topoisomerase-II inhibition. |
| AID721733 | Inhibition of rat recombinant DYRK1A-GST expressed in Escherichia coli using KKISGRLSPIMTEQ as substrate | 2013 | European journal of medicinal chemistry, Jan, Volume: 59 | Synthesis and biological evaluation of N-aryl-7-methoxybenzo[b]furo[3,2-d]pyrimidin-4-amines and their N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amine analogues as dual inhibitors of CLK1 and DYRK1A kinases. |
| AID1635798 | Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive ATPase activity at 1 uM after 20 mins by colorimetric method | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Synthesis and Investigation of Tetrahydro-β-carboline Derivatives as Inhibitors of the Breast Cancer Resistance Protein (ABCG2). |
| AID1765292 | Permeability of compound by PAMPA-BBB assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease. |
| AID1356549 | Inhibition of human CDKL5 expressed in mammalian expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID707696 | Inhibition of starfish CDK1/cyclin B using histone H1 as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1546977 | Displacement of [3H]rauwoiscine from human recombinant adrenergic alpha2A receptor expressed in CHOK1 cells at 10 uM incubated for 60 mins by radiometric enzymatic assay relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID435962 | Percentage CDK2-cyclinA activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1356579 | Inhibition of human VPS34 expressed in mammalian expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID417451 | Cytotoxicity against human HeLa cells by MTT assay | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis and in vitro cytotoxic evaluation of novel 3,4,5-trimethoxyphenyl substituted beta-carboline derivatives. |
| AID721736 | Inhibition of human recombinant CDK5/p25 after 30 mins by scintillation counting | 2013 | European journal of medicinal chemistry, Jan, Volume: 59 | Synthesis and biological evaluation of N-aryl-7-methoxybenzo[b]furo[3,2-d]pyrimidin-4-amines and their N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amine analogues as dual inhibitors of CLK1 and DYRK1A kinases. |
| AID1581637 | Antiplasmodial activity against liver stage luciferase expressing Plasmodium berghei sporozoites infected in human Huh7 cells preincubated with host cells for 1 hr followed by plasmodium infection by bioluminescence assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Harmicines - harmine and cinnamic acid hybrids as novel antiplasmodial hits. |
| AID1547005 | Binding affinity to wild-type human partial length CSNK1A1 (M1 to L450 residues) expressed in mammalian expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID36222 | Binding affinity towards Alpha-2B adrenergic receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID5996 | Binding affinity towards 5-HT3 receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID1335822 | Inhibition of GST-tagged human recombinant CLK1 expressed in Escherichia coli using RS peptide as substrate incubated for 30 mins in presence of [gamma-33 P] ATP by liquid scintillation counting analysis | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors. |
| AID722907 | Acute toxicity in ip treated C57BL/6 mouse for 14 days | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Design, synthesis and in vitro and in vivo antitumor activities of novel bivalent β-carbolines. |
| AID1762310 | Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of cell growth incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Bioinspired imidazo[1,2-a:4,5-c']dipyridines with dual antiproliferative and anti-migrative properties in human cancer cells: The SAR investigation. |
| AID653127 | Inhibition of DYRK1A | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5 | Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors. |
| AID1752117 | Inhibition of human DYRK1A-mediated tau phosphorylation expressed in HEK293 cells incubated for 2 hrs by ELISA | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15 | Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors. |
| AID707503 | Inhibition of human recombinant GSK3alpha expressed in insect cells using YRRAAVPPSPSLSRHSSPHQ-phosphoS-EDEEE as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID722894 | Antitumor activity in mouse B16 melanoma cell lines cells inoculated mouse assessed as tumor inhibition rate at one fifth of LD50 concentration once a day for consecutive 7 days by ip | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Design, synthesis and in vitro and in vivo antitumor activities of novel bivalent β-carbolines. |
| AID1266838 | Induction of DNA damage in human HCT116 cells assessed as histone H2AX phosphorylation at S139 at 20 uM after 12 hrs by western blot analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway. |
| AID1762313 | Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell viability incubated for 1 day by MTT assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Bioinspired imidazo[1,2-a:4,5-c']dipyridines with dual antiproliferative and anti-migrative properties in human cancer cells: The SAR investigation. |
| AID1415640 | Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
| AID1823479 | Antiproliferative activity against human FaDu cells assessed as reduction in cell viability at 10 uM measured after 72 hrs by Celltiter-Glo luminescent assay | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID707480 | Binding affinity to CLK3 | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1546987 | Toxicity in C57BL6N mouse assessed as induction of tremor lasting 5 to 15 mins by measuring hunched-back posture at 10 mg/kg, ip | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID4247 | Binding affinity towards 5-hydroxytryptamine 1B receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID1356573 | Inhibition of human PIK4CB expressed in mammalian expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID724335 | Cytotoxicity against human HT-29 cells by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID1226062 | Mitochondrial uncoupling activity in HEK293T/17 cells at 50 uM after 30 mins by TMRE staining-based fluorescence assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Exploiting the Polypharmacology of ß-Carbolines to Disrupt O. volvulus Molting. |
| AID697229 | Growth inhibition of human OE21 cells after 3 days by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | Novel trisubstituted harmine derivatives with original in vitro anticancer activity. |
| AID435418 | Percentage PAK5 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1823488 | Induction of apoptosis in human CAL-27 cells assessed as decrease in AKT phosphorylation at S473 residue at 5 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID3824 | Binding affinity towards 5-hydroxytryptamine 1A receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID1890952 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 65 | Synthesis of harmine-nitric oxide donor derivatives as potential antitumor agents. |
| AID1546954 | Toxicity in C57BL6N mouse assessed as induction of hyperactivity lasting 5 to 15 mins at 10 mg/kg, ip | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1581638 | Cytotoxicity against human HepG2 cells measured after 24 hrs by neutral red assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Harmicines - harmine and cinnamic acid hybrids as novel antiplasmodial hits. |
| AID707259 | Inhibition of DYRK1A in CD Sprague-Dawley rat brain assessed as inhibition of human APP-induced neurodegeneration at 4.5 to 45 uM after 3 hrs by fluorescence microscopic analysis | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1181716 | Antimicrobial activity against amastigote stage of Leishmania infantum | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Synthesis, antileishmanial and antitrypanosomal activities of N-substituted tetrahydro-β-carbolines. |
| AID625776 | Antiplatelet activity in rabbit platelets assessed as inhibition of collagen-induced platelet aggregation | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | A class of novel N-(1-methyl-β-carboline-3-carbonyl)-N'-(aminoacid-acyl)-hydrazines: aromatization leaded design, synthesis, in vitro anti-platelet aggregation/in vivo anti-thrombotic evaluation and 3D QSAR analysis. |
| AID707501 | Inhibition of pig GSK3alpha/beta isolated from brain using YRRAAVPPSPSLSRHSSPHQ-phosphoS-EDEEE as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1543970 | Induction of autophagy in human Bel7402/5-FU cells assessed as increase in red fluorescence at 20 uM incubated for 72 hrs by acridine orange staining based fluorescence microscopy | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
| AID724337 | Cytotoxicity against human A375 cells by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID1890951 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 65 | Synthesis of harmine-nitric oxide donor derivatives as potential antitumor agents. |
| AID1356538 | Inhibition of human DYRK1A | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1478469 | Antiproliferative activity against human HL60 cells by tryphan blue assay | 2017 | Journal of natural products, 02-24, Volume: 80, Issue:2 | Structurally Diverse Alkaloids from the Seeds of Peganum harmala. |
| AID435176 | Percentage PIM2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1420028 | Inhibition of human full length DYRK3 using KKISGRLSPIMTEQ as substrate after 30 mins in presence of [gamma33P-ATP] | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics. |
| AID707502 | Inhibition of human recombinant GSK3beta expressed in insect cells using YRRAAVPPSPSLSRHSSPHQ-phosphoS-EDEEE as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1823484 | Induction of apoptosis in human CAL-27 cells assessed as BCL-xL level at 1 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID435571 | Inhibition of DYRK2 in the presence of 50uM ATP | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1851170 | Inhibition of DYRK1A (unknown origin) | 2022 | Bioorganic & medicinal chemistry, 09-15, Volume: 70 | A critical update on the strategies towards small molecule inhibitors targeting Serine/arginine-rich (SR) proteins and Serine/arginine-rich proteins related kinases in alternative splicing. |
| AID1890996 | Acute toxicity in ICR mouse assessed as mortality rate at 10 mg/kg, ip measured over 14 days | 2022 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 65 | Synthesis of harmine-nitric oxide donor derivatives as potential antitumor agents. |
| AID1356576 | Inhibition of human PIP5K2C expressed in mammalian expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID707484 | Binding affinity to DYRK1A | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID417453 | Cytotoxicity against human BGC823 cells by MTT assay | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis and in vitro cytotoxic evaluation of novel 3,4,5-trimethoxyphenyl substituted beta-carboline derivatives. |
| AID1284864 | Inhibition of recombinant human N-terminal GST-tagged DYRK2 expressed in Escherichia coli BL21(DE3) cells using KKISGRLSPIMTEQ-NH2 as substrate incubated for 15 mins in presence of [gamma-32P]ATP | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2. |
| AID1859907 | Cytotoxicity against human HepG2 cells assessed as cell growth inhibition incubated for 1 day by neutral red assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents. |
| AID1105362 | Herbicidal activity against Echinochloa crus-galli (barnyard grass) assessed as growth inhibition at 10 ug/ml | 2012 | Molecules (Basel, Switzerland), Apr-02, Volume: 17, Issue:4 | Synthesis and herbicidal activity evaluation of novel β-carboline derivatives. |
| AID1823486 | Induction of apoptosis in human CAL-27 cells assessed as decrease in AKT phosphorylation at S473 residue at 0.5 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1356575 | Inhibition of human PIM2 expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID724340 | Cytotoxicity against human MCF7 cells by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID697231 | Growth inhibition of human Hs 683 cells after 3 days by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | Novel trisubstituted harmine derivatives with original in vitro anticancer activity. |
| AID550168 | Inhibition of human recombinant MAO-A expressed in baculovirus-infected Bacillus thuringiensis israelensis cells after 1 hr by two-step bioluminescent assay | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Synthesis and evaluation of β-carboline derivatives as potential monoamine oxidase inhibitors. |
| AID479485 | Displacement of bis-ANS from Plasmodium falciparum 3D7 Hsp90 expressed in Escherichia coli BL21(DE3) assessed as reduction in fluorescence at 100 uM after 30 min by fluorescent monochromator spectrophotometry | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | A repurposing strategy identifies novel synergistic inhibitors of Plasmodium falciparum heat shock protein 90. |
| AID1417232 | Cytotoxicity against human HeLa cells after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Development of novel 2,4-bispyridyl thiophene-based compounds as highly potent and selective Dyrk1A inhibitors. Part I: Benzamide and benzylamide derivatives. |
| AID724334 | Cytotoxicity against human SCaBER cells by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID655305 | Inhibition of human recombinant N-terminal MBP-tagged haspin kinase expressed in Escherichia coli DE3 after 10 mins by TR-FRET assay | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5 | Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors. |
| AID1543958 | Induction of apoptosis in human Bel7402/5-FU cells assessed as necrotic cells at 20 uM incubated for 72 hrs by FITC-Annexin V/PI staining based flow cytometry (Rvb = 2.27%) | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
| AID1769949 | Selectivity index, ratio of IC50 for human HepG2 cells to IC50 for chloroquine-resistant erythrocytic stage Plasmodium falciparum 3D7 | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Further investigation of harmicines as novel antiplasmodial agents: Synthesis, structure-activity relationship and insight into the mechanism of action. |
| AID1882206 | Antifungal activity against Bipolaris maydis relative to control | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Natural and synthetic β-carboline as a privileged antifungal scaffolds. |
| AID1627156 | Cytotoxicity against human SMMC7721 cells assessed as inhibition of cell growth after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Synthesis and biological evaluation of N(9)-substituted harmine derivatives as potential anticancer agents. |
| AID1441343 | Inhibition of full-length recombinant human GST-tagged DYRK2 expressed in Escherichia coli using woodtide as substrate after 30 mins in presence of [gamma-33P]ATP | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Structural Optimization and Pharmacological Evaluation of Inhibitors Targeting Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases (DYRK) and CDC-like kinases (CLK) in Glioblastoma. |
| AID1890948 | Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 65 | Synthesis of harmine-nitric oxide donor derivatives as potential antitumor agents. |
| AID1823489 | Induction of apoptosis in human CAL-27 cells assessed as decrease in AKT phosphorylation at S473 residue at 10 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID707499 | Inhibition of Plasmodium falciparum recombinant GSK3 expressed in Escherichia coli using YRRAAVPPSPSLSRHSSPHQ-phosphoS-EDEEE as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID697232 | Growth inhibition of human T98G cells after 3 days by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | Novel trisubstituted harmine derivatives with original in vitro anticancer activity. |
| AID606361 | Inhibition of CLK1 transfected in human HeLa cells assessed as increase in exon inclusion ratio after 24 hrs by RT-PCR analysis | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. |
| AID435713 | Percentage CHK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1403152 | Inhibition of HDAC1 (unknown origin) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
| AID707508 | Inhibition of human recombinant GST-tagged DYRK1B expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707695 | Inhibition of CDK2/cyclin A using [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID435728 | Percentage JNK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1547006 | Binding affinity to wild-type human full length CSNK1D (M1 to K409 residues) expressed in bacterial expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID223242 | Binding affinity towards Imidazoline I2 receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID1403156 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
| AID1648105 | Inhibition of GSK3beta (unknown origin) | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133. |
| AID1900711 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease. |
| AID1648107 | Induction of cell proliferation in rat beta cells relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133. |
| AID1714122 | Inhibition of human DYRK1B using [33P]-ATP incubated for 120 mins | 2016 | Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22 | An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases. |
| AID1543932 | Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
| AID1547010 | Binding affinity to wild-type human partial length DYRK1A (H129 to S509 residues) expressed in mammalian expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID435225 | Percentage DYRK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1890509 | Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects. |
| AID435256 | Percentage p38-gamma MAPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1547018 | Binding affinity to wild-type human partial length PIK3CG (S144 to A1102 residues) expressed in mammalian expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1635790 | Ratio of IC50 for human ABCG2 expressed in MDCK2 cells to GI50 for wild-type MDCK2 cells | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Synthesis and Investigation of Tetrahydro-β-carboline Derivatives as Inhibitors of the Breast Cancer Resistance Protein (ABCG2). |
| AID721730 | Inhibition of DYRK2 (unknown origin) | 2013 | European journal of medicinal chemistry, Jan, Volume: 59 | Synthesis and biological evaluation of N-aryl-7-methoxybenzo[b]furo[3,2-d]pyrimidin-4-amines and their N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amine analogues as dual inhibitors of CLK1 and DYRK1A kinases. |
| AID1546960 | Induction of beta-cell proliferation in human pancreatic islets incubated for 96 hrs by Ki67-insulin co-immunolabeling assay | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID724327 | Neurotoxicity in ip dosed C57BL/6 mouse assessed as tremble, twitch, jumping and supination response | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID1356548 | Inhibition of human CDK8 expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1356565 | Inhibition of human DYRK1B expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1203151 | Inhibition of GST-tagged Dyrk4 (unknown origin) expressed in Escherichia coli using [33P]ATP[gammaP]/DYRKtide as substrate after 5 mins by liquid scintillation counting analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis. |
| AID1546959 | Induction of beta-cell proliferation in human pancreatic islets at 10 uM incubated for 96 hrs by Ki67-insulin co-immunolabeling assay | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1356543 | Toxicity in human pancreatic islets at 10 uM | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID51723 | Inhibition of Cell division cycle 2 (CDK1)-cyclin B | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | Beta-carbolines as specific inhibitors of cyclin-dependent kinases. |
| AID72157 | In vitro cytotoxic activity tested in mouse mammary tumor FM3A cells | 2004 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 14, Issue:7 | Pi-delocalized beta-carbolinium cations as potential antimalarials. |
| AID1665600 | Induction of apoptosis in human HT-29 cells assessed as increase in cleaved caspase-3 protein level at 10 uM incubated for 72 hrs by Western blot analysis | |||
| AID435233 | Percentage HIPK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435250 | Percentage MSK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1062364 | Competitive inhibition of DYRK1A (unknown origin) using ATP | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | Development of DANDYs, new 3,5-diaryl-7-azaindoles demonstrating potent DYRK1A kinase inhibitory activity. |
| AID1467090 | Inhibition of porcine brain GSK-3 alpha/beta using YRRAAVPPSPSLSRHSSPHQpSEDEEE as substrate after 30 mins in presence of ATP by scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | N-(1H-Pyrazol-3-yl)quinazolin-4-amines as a novel class of casein kinase 1δ/ε inhibitors: Synthesis, biological evaluation and molecular modeling studies. |
| AID435613 | Percentage MNK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1203149 | Inhibition of GST-tagged Dyrk1B (unknown origin) expressed in Escherichia coli using [33P]ATP[gammaP]/DYRKtide as substrate after 5 mins by liquid scintillation counting analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis. |
| AID125789 | Inhibitory effect on Bufuralol 1'-hydroxylation by human liver microsomes (Ki = apparent inhibition constant) | 1993 | Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9 | Development of a pharmacophore for inhibition of human liver cytochrome P-450 2D6: molecular modeling and inhibition studies. |
| AID707485 | Binding affinity to CLK4 | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1356560 | Inhibition of human DAPK1 expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID752777 | Competitive inhibition of GST-tagged DYRK1A (unknown origin) expressed in Escherichia coli BL21(DE3) by Lineweaver-Burk plot analysis in presence of ATP | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12 | Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315. |
| AID1478838 | Induction of nuclear translocation of human GFP-tagged NFATc1 expressed in virus infected primary human skeletal muscle myoblasts after 3 hrs by DAPI staining based assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Developing DYRK inhibitors derived from the meridianins as a means of increasing levels of NFAT in the nucleus. |
| AID72269 | Inhibition of Fyn kinase | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | Beta-carbolines as specific inhibitors of cyclin-dependent kinases. |
| AID1284955 | Growth inhibition of human U87MG cells after 4 days by MTT assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2. |
| AID1356572 | Inhibition of human IRAK3 expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1493939 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis and biological evaluation of new β-carboline-bisindole compounds as DNA binding, photocleavage agents and topoisomerase I inhibitors. |
| AID435756 | Percentage Src activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1665604 | Induction of autophagy in human HT-29 cells assessed as increase in LC3-II protein level at 10 uM incubated for 72 hrs by Western blot analysis | |||
| AID436071 | Percentage CHK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1284865 | Inhibition of CK2 (unknown origin) using RRRDDDSDDD-NH2 as susbtrate incubated for 15 mins in presence of [gamma-32P]ATP | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2. |
| AID658629 | Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition after 24 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Solvent effect on copper-catalyzed azide-alkyne cycloaddition (CuAAC): synthesis of novel triazolyl substituted quinolines as potential anticancer agents. |
| AID1823485 | Induction of apoptosis in human CAL-27 cells assessed as BCL-xL level at 10 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1823462 | Inhibition of DYRK1A (unknown origin) measured after 6 hrs in presence of ATP by Z'-LYTE assay | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID658625 | Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 24 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Solvent effect on copper-catalyzed azide-alkyne cycloaddition (CuAAC): synthesis of novel triazolyl substituted quinolines as potential anticancer agents. |
| AID36487 | Binding affinity towards Alpha-1A adrenergic receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID1546976 | Inhibition of human recombinant MAOA expressed in insect cells at 10 uM pre-incubated for 15 mins before kynuramine addition and measured after 60 mins by radiometric enzymatic assay relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1665594 | Induction of apoptosis in human HT-29 cells assessed as increase in Bax protein level at 10 uM incubated for 72 hrs by Western blot analysis | |||
| AID435238 | Percentage JNK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID707509 | Inhibition of human recombinant C-terminal truncated GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID724329 | Cytotoxicity against human KB cells by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID1762311 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Bioinspired imidazo[1,2-a:4,5-c']dipyridines with dual antiproliferative and anti-migrative properties in human cancer cells: The SAR investigation. |
| AID1181720 | Antimicrobial activity against promastigote stage of Leishmania donovani after 72 hrs by Alamar Blue assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Synthesis, antileishmanial and antitrypanosomal activities of N-substituted tetrahydro-β-carbolines. |
| AID1417151 | Binding affinity to full length human DYRK1B (M1 to S629 residues) expressed in bacterial expression system assessed as remaining unbound target protein level at 10 uM by Kinomescan method relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel selective thiadiazine DYRK1A inhibitor lead scaffold with human pancreatic β-cell proliferation activity. |
| AID721732 | Inhibition of human recombinant CLK1-GST expressed in Escherichia coli using GRSRSRSRSRSR as substrate | 2013 | European journal of medicinal chemistry, Jan, Volume: 59 | Synthesis and biological evaluation of N-aryl-7-methoxybenzo[b]furo[3,2-d]pyrimidin-4-amines and their N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amine analogues as dual inhibitors of CLK1 and DYRK1A kinases. |
| AID5536 | Binding affinity towards 5-hydroxytryptamine 2A receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID1917481 | Inhibition of human recombinant MAO-A assessed as inhibition of 4-hydroxyquinoline formation using kynuramine as substrate incubated for 20 mins by fluorescence spectrophotometry | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Isatoic anhydrides as novel inhibitors of monoamine oxidase. |
| AID435334 | Inhibition of DYRK3 in the presence of 50uM ATP | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1547016 | Binding affinity to wild-type human partial length IRAK1 (R194 to S712 residues) expressed in mammalian expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1441345 | Inhibition of recombinant GST-tagged DYRK1B (unknown origin) expressed in Escherichia coli using DYRKtide as substrate after 5 mins in presence of [gamma-33P]ATP by liquid scintillation counting | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Structural Optimization and Pharmacological Evaluation of Inhibitors Targeting Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases (DYRK) and CDC-like kinases (CLK) in Glioblastoma. |
| AID435738 | Percentage p38delta MAPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID636106 | Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Ultrasound mediated catalyst free synthesis of 6H-1-benzopyrano[4,3-b]quinolin-6-ones leading to novel quinoline derivatives: their evaluation as potential anti-cancer agents. |
| AID697228 | Inhibition of human DYRK1A kinase expressed in Escherichia coli cells | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | Novel trisubstituted harmine derivatives with original in vitro anticancer activity. |
| AID435842 | Percentage Aurora C activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435669 | Percentage PDK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435375 | Percentage RSK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1420027 | Inhibition of human full length DYRK2 using KKISGRLSPIMTEQ as substrate after 30 mins in presence of [gamma33P-ATP] | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics. |
| AID1578920 | Inhibition of PI3K/AKT/mTOR signaling in human Bel7402 cells assessed as reduction in AKT phosphorylation at 20 uM after 24 to 72 hrs by Western blot analysis | 2019 | Journal of natural products, 06-28, Volume: 82, Issue:6 | Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways. |
| AID1547002 | Binding affinity to wild-type human full length CLK1 (M1 to I484 residues) expressed in bacterial expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1546983 | Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT7 receptor expressed in CHOK1 cells at 10 uM incubated for 2 hrs by radiometric enzymatic assay relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID224144 | Inhibition of Lyn tyrosine kinase | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | Beta-carbolines as specific inhibitors of cyclin-dependent kinases. |
| AID1546988 | Toxicity in C57BL6N mouse assessed as effect on normal ambulation at 10 mg/kg, ip | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1415638 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
| AID1588122 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15 | Synthesis and in vitro cytotoxicity evaluation of β-carboline-combretastatin carboxamides as apoptosis inducing agents: DNA intercalation and topoisomerase-II inhibition. |
| AID1335820 | Inhibition of porcine brain GSK3alpha/beta using GS-1 as substrate incubated for 30 mins in presence of [gamma-33 P] ATP by liquid scintillation counting analysis | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors. |
| AID697226 | Cytostatic activity in human U373 cells at 32 uM assessed global growth ratio after 72 hrs by quantitative video microscopy | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | Novel trisubstituted harmine derivatives with original in vitro anticancer activity. |
| AID1622954 | Inhibition of HDAC in human HeLa nuclear extract | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors. |
| AID1546979 | Displacement of [3H]rauwoiscine from human recombinant adrenergic alpha2C receptor expressed in CHOK1 cells at 10 uM incubated for 60 mins by radiometric enzymatic assay relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID435417 | Percentage PAK4 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID722895 | Antitumor activity in mouse Sarcoma 180 cells inoculated mouse assessed as tumor inhibition rate at one fifth of LD50 concentration once a day for consecutive 7 days by ip | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Design, synthesis and in vitro and in vivo antitumor activities of novel bivalent β-carbolines. |
| AID1627157 | Cytotoxicity against human A549 cells assessed as inhibition of cell growth after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Synthesis and biological evaluation of N(9)-substituted harmine derivatives as potential anticancer agents. |
| AID435820 | Percentage PKCalpha activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID707500 | Inhibition of human recombinant PIM1 expressed in Escherichia coli using histone H1 as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1665596 | Induction of apoptosis in human HT-29 cells assessed as reduction in Bcl2 protein level at 10 uM incubated for 72 hrs by Western blot analysis | |||
| AID722906 | Neurotoxicity in C57BL/6 mouse at 1 to 500 mg/kg, ip for 14 days | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Design, synthesis and in vitro and in vivo antitumor activities of novel bivalent β-carbolines. |
| AID1627154 | Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Synthesis and biological evaluation of N(9)-substituted harmine derivatives as potential anticancer agents. |
| AID722911 | Cytotoxicity against human malignant melanoma A375 cells assessed as reduction in optical density by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Design, synthesis and in vitro and in vivo antitumor activities of novel bivalent β-carbolines. |
| AID722910 | Cytotoxicity against human renal carcinoma 769-P cells assessed as reduction in optical density by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Design, synthesis and in vitro and in vivo antitumor activities of novel bivalent β-carbolines. |
| AID1415637 | Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 60 mins by fluorescence assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
| AID1493940 | Antiproliferative activity against mouse NIH/3T3 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis and biological evaluation of new β-carboline-bisindole compounds as DNA binding, photocleavage agents and topoisomerase I inhibitors. |
| AID707687 | Inhibition of mouse recombinant GST-tagged CLK3 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1882205 | Antifungal activity against Alternaria solani relative to control | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Natural and synthetic β-carboline as a privileged antifungal scaffolds. |
| AID435317 | Percentage PIM1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID649864 | Antiproliferative activity against human K562 cells after 24 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6 | Catalysis by molecular iodine: a rapid synthesis of 1,8-dioxo-octahydroxanthenes and their evaluation as potential anticancer agents. |
| AID54179 | Inhibition of Cyclin-dependent kinase 5-p35nck5a | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | Beta-carbolines as specific inhibitors of cyclin-dependent kinases. |
| AID42569 | In vitro cytotoxic activity was determined against renal cancer (CAKI-1) cell line | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Antitumor agents 201. Cytotoxicity of harmine and beta-carboline analogs. |
| AID656684 | Inhibition of human AChE by Ellman's method | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Prospective acetylcholinesterase inhibitory activity of indole and its analogs. |
| AID724332 | Cytotoxicity against human Blu-87 cells by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID1415656 | Binding affinity to calf thymus DNA assessed as maximum absorption wavelength by UV-Vis spectroscopic titration method | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
| AID435339 | Percentage CaMKKbeta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1765290 | Inhibition of rat recombinant DYRK1A expressed in Escherichia coli using RRRFRPASPLRGPPK as substrate at 10 uM by ADP-Glo kinase assay relative to control | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease. |
| AID1356536 | Inhibition of GST-tagged human recombinant DYRK1A at 300 nM by FRET-based LanthaScreen Eu kinase binding assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID697230 | Growth inhibition of human OE33 cells after 3 days by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | Novel trisubstituted harmine derivatives with original in vitro anticancer activity. |
| AID435350 | Percentage ERK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID550169 | Inhibition of human recombinant MAO-B expressed in baculovirus-infected Bacillus thuringiensis israelensis cells after 1 hr by two-step bioluminescent assay | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Synthesis and evaluation of β-carboline derivatives as potential monoamine oxidase inhibitors. |
| AID1890950 | Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 65 | Synthesis of harmine-nitric oxide donor derivatives as potential antitumor agents. |
| AID1859902 | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 assessed as inhibition of parasite growth incubated for 3 days by HRP2-ELISA | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents. |
| AID1226059 | Competitive inhibition of L3 larval stage of Onchocerca volvulus chitinase using 4-methylumbelliferyl-N-N'-N''-beta-chitotrioside as substrate assessed as release of 4-methylumbelliferone measured for 10 mins by Dixon plot analysis | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Exploiting the Polypharmacology of ß-Carbolines to Disrupt O. volvulus Molting. |
| AID311934 | Dissociation constant, pKa of the compound | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. |
| AID1765289 | Inhibition of human full length GSK3beta expressed in baculovirus in Sf9 insect cells using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate by ADP-Glo kinase assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease. |
| AID1203169 | Inhibition of Dyrk1B (unknown origin) autophosphorylation at Y273 | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis. |
| AID1635778 | Cytotoxicity against wild-type MDCK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Synthesis and Investigation of Tetrahydro-β-carboline Derivatives as Inhibitors of the Breast Cancer Resistance Protein (ABCG2). |
| AID435541 | Percentage PKA activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1165915 | Inhibition of CDK5/p25 (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21 | Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors. |
| AID435995 | Percentage SRPK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1062356 | Selectivity for rat recombinant 6xHis-tagged DYRK1A catalytic domain (1 to 502) over human DYRK3 | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | Development of DANDYs, new 3,5-diaryl-7-azaindoles demonstrating potent DYRK1A kinase inhibitory activity. |
| AID1823487 | Induction of apoptosis in human CAL-27 cells assessed as decrease in AKT phosphorylation at S473 residue at 1 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1356569 | Inhibition of human HIPK2 expressed in mammalian expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1859901 | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum Dd2 assessed as inhibition of parasite growth incubated for 3 days by HRP2-ELISA | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents. |
| AID435681 | Percentage MAPKAPK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1547009 | Binding affinity to wild-type human full length CSNK2A1 (M1 to Q391 residues) expressed in mammalian expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1665585 | Induction of apoptosis in human HT-29 cells at 10 uM incubated for 72 hrs by FITC-AnnexinV/PI staining based flow cytometry relative to control | |||
| AID436086 | Percentage HIPK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1545859 | Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
| AID977599 | Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID1403158 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
| AID653128 | Selectivity ratio of IC50 for DYRK2 to IC50 for DYRK1A | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5 | Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors. |
| AID435223 | Percentage CSK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1266812 | Antiproliferative activity against human LoVo cells assessed as cell viability after 48 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway. |
| AID1543952 | Induction of apoptosis in human Bel7402/5-FU cells assessed as early apoptotic cells at 20 uM incubated for 72 hrs by FITC-Annexin V/PI staining based flow cytometry (Rvb =3.60%) | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
| AID1415641 | Antiproliferative activity against human LoVo cells after 48 hrs by MTT assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with DNA damage and apoptosis inducing abilities. |
| AID1266810 | Antiproliferative activity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Novel β-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway. |
| AID1665605 | Induction of autophagy in human HT-29 cells assessed as increase in Beclin-1 protein level at 10 uM incubated for 72 hrs by Western blot analysis | |||
| AID36400 | Binding affinity towards Alpha-2C adrenergic receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID1335818 | Inhibition of porcine brain CK1 delta/epsilon using RRKHAAIGpSAYSITA as substrate incubated for 30 mins in presence of [gamma-33 P] ATP by liquid scintillation counting analysis | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors. |
| AID1823493 | Induction of apoptosis in human CAL-27 cells assessed as decrease in FOXO3A phosphorylation at serine 253 residue at 10 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID417452 | Cytotoxicity against human Bel7402 cells by MTT assay | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Synthesis and in vitro cytotoxic evaluation of novel 3,4,5-trimethoxyphenyl substituted beta-carboline derivatives. |
| AID160056 | In vitro antimalarial activity against Plasmodium falciparum FCR3 | 2004 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 14, Issue:7 | Pi-delocalized beta-carbolinium cations as potential antimalarials. |
| AID1578882 | Antiproliferative activity against human SMMC7721 cells after 72 hrs by MTT assay | 2019 | Journal of natural products, 06-28, Volume: 82, Issue:6 | Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways. |
| AID707684 | Inhibition of rat DYRK1A isolated from brain using KKISGRLSPIMTEQ as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1765291 | Inhibition of rat recombinant DYRK1A expressed in Escherichia coli using RRRFRPASPLRGPPK as substrate at 1 uM by ADP-Glo kinase assay | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease. |
| AID1547019 | Binding affinity to wild-type human full length PIK4CB (M1 to M828 residues) expressed in mammalian expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID707685 | Inhibition of rat recombinant C-terminal truncated GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID35941 | Binding affinity towards alpha-2A-Adrenergic receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID1758385 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Discovery of β-carboline-(phenylsulfonyl)furoxan hybrids as potential anti-breast cancer agents. |
| AID1181721 | Antimicrobial activity against axenic amastigote stage of Leishmania donovani after 72 hrs by Alamar Blue assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Synthesis, antileishmanial and antitrypanosomal activities of N-substituted tetrahydro-β-carbolines. |
| AID1546986 | Toxicity in C57BL6N mouse assessed as induction of tremor lasting 5 to 15 mins by measuring Straub tail phenomenon at 10 mg/kg, ip | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1226063 | Antionchocerciasis activity against L3 larval stage of Onchocerca volvulus assessed as inhibition of parasite molting at 10 uM treated for 24 hrs prior to complete medium and PBMC addition measured after 6 days by inverted microscopic analysis | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Exploiting the Polypharmacology of ß-Carbolines to Disrupt O. volvulus Molting. |
| AID707691 | Inhibition of pig CD1delta/epsilon isolated from brain using RRKHAAIGpSAYSITA as substrate and [gamma33P]ATP after 30 mins by scintillation couting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1432637 | Cytotoxicity against human COLO205 cells assessed as decrease in cell viability after 24 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6 | Synthesis of novel spiro[pyrazolo[4,3-d]pyrimidinones and spiro[benzo[4,5]thieno[2,3-d]pyrimidine-2,3'-indoline]-2',4(3H)-diones and their evaluation for anticancer activity. |
| AID435979 | Percentage MST2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1581635 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 erythrocytic stage measured after 3 days by HRP2 assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Harmicines - harmine and cinnamic acid hybrids as novel antiplasmodial hits. |
| AID435621 | Percentage p38alpha MAPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1588123 | Antiproliferative activity against human DU145 cells assessed as reduction in cell viability after 48 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15 | Synthesis and in vitro cytotoxicity evaluation of β-carboline-combretastatin carboxamides as apoptosis inducing agents: DNA intercalation and topoisomerase-II inhibition. |
| AID436072 | Percentage CK1delta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID707694 | Inhibition of human recombinant CDK5/p25 using histone H1 as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1547011 | Binding affinity to wild-type human full length DYRK1B (M1 to S629 residues) expressed in bacterial expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID8467 | In vitro cytotoxic activity was determined against lung carcinoma (A549) cell line | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Antitumor agents 201. Cytotoxicity of harmine and beta-carboline analogs. |
| AID707686 | Inhibition of mouse recombinant GST-tagged CLK4 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID435450 | Inhibition of CK1delta in the presence of 20uM ATP | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435987 | Percentage PRK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1769945 | Antiplasmodial activity against chloroquine-sensitive erythrocytic stage Plasmodium falciparum 3D7 assessed as inhibition of parasite growth incubated for 3 days by HRP2-ELISA | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Further investigation of harmicines as novel antiplasmodial agents: Synthesis, structure-activity relationship and insight into the mechanism of action. |
| AID724328 | Acute toxicity in ip dosed C57BL/6 mouse measured up to 14 days | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID673517 | Antiproliferative activity against human MDA-MB-231 cells by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15 | InCl3-catalysed synthesis of 2-aryl quinazolin-4(3H)-ones and 5-aryl pyrazolo[4,3-d]pyrimidin-7(6H)-ones and their evaluation as potential anticancer agents. |
| AID1330647 | Inhibition of GSK-3 alpha/beta (unknown origin) | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis, biological evaluation and molecular modeling studies of imidazo[1,2-a]pyridines derivatives as protein kinase inhibitors. |
| AID724339 | Cytotoxicity against human OS-RC2 cells by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID435847 | Percentage DYRK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435363 | Percentage MELK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1823483 | Induction of apoptosis in human CAL-27 cells assessed as PARP level at 10 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1417150 | Binding affinity to wild-type human partial length DYRK1A (H129 to S509 residues) expressed in mammalian expression system assessed as remaining unbound target protein level at 10 uM by Kinomescan method relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel selective thiadiazine DYRK1A inhibitor lead scaffold with human pancreatic β-cell proliferation activity. |
| AID1578885 | Antiproliferative activity against human HuH7 cells after 72 hrs by MTT assay | 2019 | Journal of natural products, 06-28, Volume: 82, Issue:6 | Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways. |
| AID1420029 | Inhibition of DYRK1A in human HeLa cells assessed as decrease in SF3B1 phosphorylation at Thr434 after 48 hrs by Western blot analysis | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics. |
| AID1543961 | Induction of apoptosis in human Bel7402/5-FU cells assessed as live cells at 20 uM incubated for 72 hrs by FITC-Annexin V/PI staining based flow cytometry (Rvb = 93.12%) | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | β-Carboline and N-hydroxycinnamamide hybrids as anticancer agents for drug-resistant hepatocellular carcinoma. |
| AID649863 | Antiproliferative activity against human COLO205 cells after 24 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6 | Catalysis by molecular iodine: a rapid synthesis of 1,8-dioxo-octahydroxanthenes and their evaluation as potential anticancer agents. |
| AID436076 | Percentage DYRK1A activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435718 | Percentage EF2K activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1635789 | Ratio of IC50 for human ABCG2 expressed in MDCK2 cells to GI50 for MDCK2 cells expressing human ABCG2 | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Synthesis and Investigation of Tetrahydro-β-carboline Derivatives as Inhibitors of the Breast Cancer Resistance Protein (ABCG2). |
| AID435731 | Percentage MNK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1578883 | Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay | 2019 | Journal of natural products, 06-28, Volume: 82, Issue:6 | Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways. |
| AID1635779 | Cytotoxicity against MDCK2 cells expressing human ABCG2 assessed as reduction in cell viability after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Synthesis and Investigation of Tetrahydro-β-carboline Derivatives as Inhibitors of the Breast Cancer Resistance Protein (ABCG2). |
| AID707692 | Inhibition of human recombinant CDK9/cyclin T expressed in insect cell using YSPTSPSYSPTSPSYSPTSPSKKKK as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1226058 | Inhibition of L3 larval stage of Onchocerca volvulus chitinase using 4-methylumbelliferyl-N-N'-N''-beta-chitotrioside as substrate assessed as release of 4-methylumbelliferone measured for 10 mins by fluorescence assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Exploiting the Polypharmacology of ß-Carbolines to Disrupt O. volvulus Molting. |
| AID435881 | Percentage ROCK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID724331 | Cytotoxicity against human U251 cells by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID1467083 | Inhibition of M-phase starfish oocytes CDK1/cyclin B using histone H1 as substrate after 30 mins in presence of ATP by scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | N-(1H-Pyrazol-3-yl)quinazolin-4-amines as a novel class of casein kinase 1δ/ε inhibitors: Synthesis, biological evaluation and molecular modeling studies. |
| AID722896 | Antitumor activity in mouse Lewis lung cancer cells inoculated mouse assessed as tumor inhibition rate at one fifth of LD50 concentration once a day for consecutive 7 days by ip | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Design, synthesis and in vitro and in vivo antitumor activities of novel bivalent β-carbolines. |
| AID1547004 | Binding affinity to wild-type human partial length CLK4 (R135 to K481 residues) expressed in bacterial expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1062357 | Selectivity for rat recombinant 6xHis-tagged DYRK1A catalytic domain (1 to 502) over human DYRK2 | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | Development of DANDYs, new 3,5-diaryl-7-azaindoles demonstrating potent DYRK1A kinase inhibitory activity. |
| AID213899 | In vitro cytotoxic activity against U-87-MG (glioblastoma) cell line. | 1999 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23 | Antitumor agents 201. Cytotoxicity of harmine and beta-carboline analogs. |
| AID1635793 | Reversal of human ABCG2-mediated resistance to SN-38 in human ABCG2 expressed MDCK2 cells assessed as SN-38 GI50 at 1 uM after 72 hrs by MTT assay (Rvb SN-38 alone GI50 = 2.28 +/- 0.39 uM) | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Synthesis and Investigation of Tetrahydro-β-carboline Derivatives as Inhibitors of the Breast Cancer Resistance Protein (ABCG2). |
| AID435819 | Percentage PKBbeta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1284868 | Inhibition of PKCbeta (unknown origin) incubated for 15 mins in presence of [gamma-32P]ATP | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2. |
| AID436083 | Percentage ERK8 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1356551 | Inhibition of human CLK1 expressed in bacterial expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID435865 | Percentage MKK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1823481 | Inhibition of colony formation in human CAL-27 cells at 1 to 10 uM measured after 10 days by crystal violet staining based assay | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID722909 | Cytotoxicity against human epidermoid carcinoma of the nasopharynx KB cells assessed as reduction in optical density by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Design, synthesis and in vitro and in vivo antitumor activities of novel bivalent β-carbolines. |
| AID1284956 | Inhibition of tetracycline-inducible EGFP-DYRK1A (unknown origin) expressed in HEK293 cells coexpressing full length human EGFP-tau protein assessed as reduction in tau-Thr212 phosphorylation incubated overnight by immunofluorescence assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2. |
| AID1546981 | Displacement of [3H]mesulergine from human recombinant 5HT2C receptor expressed in CHOK1 cells at 10 uM incubated for 60 mins by radiometric enzymatic assay relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1888249 | Neuroprotective activity against alpha-syn induced cytotoxicity against human SH-SY5Y cells assessed as increase in cell viability at 1 to 10 uM by MTT assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Discovery of novel 6-hydroxybenzothiazole urea derivatives as dual Dyrk1A/α-synuclein aggregation inhibitors with neuroprotective effects. |
| AID1823458 | Induction of apoptosis in human CAL-27 cells assessed as increase in cleaved-PARP level at 1 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID1547017 | Binding affinity to wild-type human partial length IRAK3 (V147 to E596 residues) expressed in bacterial expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID1882232 | Inhibition of N-terminal GST-fused full-length human DYRK1A (1 to 763 residues) expressed in baculovirus expression system using myelin basic protein peptide as substrate preincubated with substrate for 40 mins followed by compound addition measured after | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | DYRK1A inhibitors for disease therapy: Current status and perspectives. |
| AID435883 | Percentage SGK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID724336 | Cytotoxicity against human 786-0 cells by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents. |
| AID1335821 | Inhibition of GST-tagged human recombinant DYRK1A expressed in Escherichia coli using RS peptide as substrate incubated for 30 mins in presence of [gamma-33 P] ATP by liquid scintillation counting analysis | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors. |
| AID41506 | Binding affinity towards Beta-2A adrenergic receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID707702 | Inhibition of mouse recombinant GST-tagged CLK1 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID636104 | Cytotoxicity against human K562 cells after 24 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Ultrasound mediated catalyst free synthesis of 6H-1-benzopyrano[4,3-b]quinolin-6-ones leading to novel quinoline derivatives: their evaluation as potential anti-cancer agents. |
| AID1356559 | Inhibition of human CSNK2A2 expressed in mammalian expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID311935 | Partition coefficient, log P of the compound | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. |
| AID1823482 | Induction of apoptosis in human CAL-27 cells assessed as PARP level at 1 uM after 24 hrs by Immunoblot analysis relative to control | 2022 | ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4 | Selective Macrocyclic Inhibitors of DYRK1A/B. |
| AID721731 | Inhibition of DYRK1A (unknown origin) | 2013 | European journal of medicinal chemistry, Jan, Volume: 59 | Synthesis and biological evaluation of N-aryl-7-methoxybenzo[b]furo[3,2-d]pyrimidin-4-amines and their N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amine analogues as dual inhibitors of CLK1 and DYRK1A kinases. |
| AID1758386 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Discovery of β-carboline-(phenylsulfonyl)furoxan hybrids as potential anti-breast cancer agents. |
| AID1578886 | Inhibition of HDAC1 (unknown origin) using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay | 2019 | Journal of natural products, 06-28, Volume: 82, Issue:6 | Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways. |
| AID64344 | Binding affinity towards DAT (bovine) | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID435704 | Percentage Aurora B activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1648106 | Induction of cell proliferation in rat beta cells | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133. |
| AID6500 | Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18 | Binding of tetrahydrocarboline derivatives at human 5-HT5A receptors. |
| AID55535 | Percentage inhibition against cyclin dependent kinase 2 (CDK 2) at a concentration of 50 uM | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | Beta-carbolines as specific inhibitors of cyclin-dependent kinases. |
| AID1820103 | Inhibition of DYRK1A (unknown origin) using Ulight-MBP as substrate and ATP as co-substrate incubated for 40 mins and measured after 1 hr by TR-FRET assay | 2021 | Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10 | Structure-Guided Discovery of Potent and Selective DYRK1A Inhibitors. |
| AID1226060 | Inhibition of Entamoeba histolytica chitinase using 4-methylumbelliferyl-N-N'-N''-beta-chitotrioside as substrate assessed as release of 4-methylumbelliferone at 10 uM measured for 10 mins by fluorescence assay | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Exploiting the Polypharmacology of ß-Carbolines to Disrupt O. volvulus Molting. |
| AID435727 | Percentage JNK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1888251 | Neuroprotective activity against 6-OHDA induced cytotoxicity against human SH-SY5Y cells assessed as increase in cell viability at 10 uM by MTT assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Discovery of novel 6-hydroxybenzothiazole urea derivatives as dual Dyrk1A/α-synuclein aggregation inhibitors with neuroprotective effects. |
| AID707688 | Inhibition of mouse recombinant GST-tagged CLK2 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID707506 | Inhibition of human recombinant GST-tagged DYRK3 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID435228 | Percentage ERK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435215 | Percentage AMPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435454 | Percentage CaMKKalpha activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435501 | Percentage SmMLCK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1203148 | Inhibition of GST-tagged Dyrk1A (unknown origin) expressed in Escherichia coli using [33P]ATP[gammaP]/DYRKtide as substrate after 5 mins by liquid scintillation counting analysis | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis. |
| AID673515 | Antiproliferative activity against human K562 cells by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15 | InCl3-catalysed synthesis of 2-aryl quinazolin-4(3H)-ones and 5-aryl pyrazolo[4,3-d]pyrimidin-7(6H)-ones and their evaluation as potential anticancer agents. |
| AID1762312 | Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Bioinspired imidazo[1,2-a:4,5-c']dipyridines with dual antiproliferative and anti-migrative properties in human cancer cells: The SAR investigation. |
| AID1284863 | Inhibition of full length recombinant human GST-tagged DYRK1B expressed in insect cells using KKISGRLSPIMTEQ-NH2 as substrate incubated for 15 mins in presence of [gamma-32P]ATP | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2. |
| AID1635783 | Inhibition of human ABCG2 expressed in MDCK2 cells assessed as reduction in pheophorbide A efflux pre-incubated for 30 mins before Hoechst 33342 addition and measured for 120 mins by flow cytometry | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Synthesis and Investigation of Tetrahydro-β-carboline Derivatives as Inhibitors of the Breast Cancer Resistance Protein (ABCG2). |
| AID1201057 | Cytostatic activity against human Hs683 cells after 72 hrs by videomicroscopy | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | 3D-QSAR, design, synthesis and characterization of trisubstituted harmine derivatives with in vitro antiproliferative properties. |
| AID1403157 | Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells. |
| AID722898 | Toxicity in C57BL/6 mouse assessed as maximum weight loss at 7.5 mg/kg, ip | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Design, synthesis and in vitro and in vivo antitumor activities of novel bivalent β-carbolines. |
| AID1237105 | Inhibition of Dyrk1A (unknown origin) using dynatide 3 as substrate after 10 mins by P81 membrane assay in presence of [33P]-g-ATP | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15 | Meridianin derivatives as potent Dyrk1A inhibitors and neuroprotective agents. |
| AID611923 | Inhibition of MAO-A | 2011 | Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15 | Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators. |
| AID1356540 | Induction of beta-cell proliferation in human pancreatic islets at 10 uM incubated for 96 hrs by Ki67 and insulin immunolabelling method | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID479488 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human erythrocytes after 48 hrs by flow-cytometry | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | A repurposing strategy identifies novel synergistic inhibitors of Plasmodium falciparum heat shock protein 90. |
| AID722912 | Cytotoxicity against human gastric carcinoma BGC823 cells assessed as reduction in optical density by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Design, synthesis and in vitro and in vivo antitumor activities of novel bivalent β-carbolines. |
| AID1547001 | Binding affinity to wild-type human full length CDK7 (M1 to L344 residues) expressed in mammalian expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID707689 | Inhibition of human recombinant CK2 using RRREDEESDDEE as substrate and [gamma33P]ATP at 10 uM after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1665557 | Antiproliferative activity against human HepG2 cells by MTT assay | |||
| AID1091974 | Insecticidal activity against Lipaphis erysimi (mustard aphids) assessed as increase in mortality at 50 to 200 mg/L after 24 to 48 hr | 2010 | Molecules (Basel, Switzerland), Nov-02, Volume: 15, Issue:11 | Cytotoxic and insecticidal activities of derivatives of harmine, a natural insecticidal component isolated from Peganum harmala. |
| AID1330646 | Inhibition of CK1 delta/epsilon (unknown origin) | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis, biological evaluation and molecular modeling studies of imidazo[1,2-a]pyridines derivatives as protein kinase inhibitors. |
| AID1356566 | Inhibition of human DYRK2 expressed in mammalian expression system assessed as remaining enzyme activity at 10 uM by kinome scan assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation. |
| AID1578921 | Inhibition of PI3K/AKT/mTOR signaling in human Bel7402 cells assessed as reduction in mTOR phosphorylation at 20 uM after 24 to 72 hrs by Western blot analysis | 2019 | Journal of natural products, 06-28, Volume: 82, Issue:6 | Hydroxamic Acid Derivatives of β-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways. |
| AID636107 | Cytotoxicity against human IMR32 cells after 24 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Ultrasound mediated catalyst free synthesis of 6H-1-benzopyrano[4,3-b]quinolin-6-ones leading to novel quinoline derivatives: their evaluation as potential anti-cancer agents. |
| AID224133 | Inhibition of p56 Lck tyrosine kinase | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | Beta-carbolines as specific inhibitors of cyclin-dependent kinases. |
| AID204092 | Binding affinity towards Serotonin transporter | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID1493936 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis and biological evaluation of new β-carboline-bisindole compounds as DNA binding, photocleavage agents and topoisomerase I inhibitors. |
| AID1882176 | Antifungal activity against Candida albicans incubated for 72 hrs | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Natural and synthetic β-carboline as a privileged antifungal scaffolds. |
| AID435814 | Percentage PIM3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID649862 | Antiproliferative activity against human IMR32 cells after 24 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6 | Catalysis by molecular iodine: a rapid synthesis of 1,8-dioxo-octahydroxanthenes and their evaluation as potential anticancer agents. |
| AID142901 | Binding affinity towards Muscarinic acetylcholine receptor | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
| AID311932 | Inhibition of ASM in human H4 cells assessed as residual activity at 10 uM | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. |
| AID1547020 | Binding affinity to wild-type human partial length VPS34 (S282 to H879 residues) expressed in mammalian expression system assessed as residual bound protein level at 10 uM by Kinomescan method relative to control | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
| AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
| AID1159550 | Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening | 2015 | Nature cell biology, Nov, Volume: 17, Issue:11 | 6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling. |
| 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. |
| AID1745854 | NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| AID1745855 | NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| 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. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
| AID1478470 | Antiproliferative activity against human PC3 cells by MTT assay | 2017 | Journal of natural products, 02-24, Volume: 80, Issue:2 | Structurally Diverse Alkaloids from the Seeds of Peganum harmala. |
| AID1478471 | Antiproliferative activity against human SGC7901 cells by MTT assay | 2017 | Journal of natural products, 02-24, Volume: 80, Issue:2 | Structurally Diverse Alkaloids from the Seeds of Peganum harmala. |
| AID1345681 | Human dual specificity tyrosine phosphorylation regulated kinase 1A (Dyrk1 subfamily) | 2009 | The FEBS journal, Nov, Volume: 276, Issue:21 | Harmine specifically inhibits protein kinase DYRK1A and interferes with neurite formation. |
| AID1345686 | Human dual specificity tyrosine phosphorylation regulated kinase 1B (Dyrk1 subfamily) | 2009 | The FEBS journal, Nov, Volume: 276, Issue:21 | Harmine specifically inhibits protein kinase DYRK1A and interferes with neurite formation. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2010 | Nature communications, Oct-05, Volume: 1 | Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 216 (22.83) | 18.7374 |
| 1990's | 107 (11.31) | 18.2507 |
| 2000's | 190 (20.08) | 29.6817 |
| 2010's | 304 (32.14) | 24.3611 |
| 2020's | 129 (13.64) | 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 strong demand-to-supply ratio for research on this compound.
| This Compound (49.55) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 11 (1.10%) | 5.53% |
| Reviews | 36 (3.60%) | 6.00% |
| Case Studies | 2 (0.20%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 952 (95.10%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| Mindfulness and Psychedelics: A Combined Neurophenomenological and Pharmacological Approach to the Characterization of Mindfulness States in Experienced Meditators [NCT05780216] | Early Phase 1 | 40 participants (Actual) | Interventional | 2023-02-20 | Completed | ||
| Single-blind, Randomized, Two-arm, Dose-response Study of DMT and Harmine in Healthy Subjects [NCT05829603] | Phase 1 | 16 participants (Actual) | Interventional | 2023-05-05 | Completed | ||
| A Phase I Dose Escalation Study of Harmine in Healthy Subjects [NCT05526430] | Phase 1 | 27 participants (Actual) | Interventional | 2022-09-13 | Completed | ||
| Effects of Electroconvulsive Therapy on Monoamine Oxidase A Distribution Volume in Treatment-Resistant Depression Investigated With PET [NCT02379767] | 27 participants (Actual) | Observational | 2015-03-31 | Completed | |||
| Neurodynamics of Prosocial Emotional Processing Following Serotonergic Stimulation With N,N-Dimethyltryptamine (DMT) and Harmine in Healthy Subjects [NCT04716335] | Early Phase 1 | 34 participants (Actual) | Interventional | 2020-12-01 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||