Page last updated: 2024-11-12
3,9-bis((ethylthio)methyl)-k-252a
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Description
3,9-bis((ethylthio)methyl)-K-252a: RN given for (9S-(9alpha,10beta,12alpha))-isomer; mixed lineage kinase inhibitor, neuroprotective agent, and neurotrophic agent derived from K-252a; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 9917013 |
| CHEMBL ID | 290352 |
| SCHEMBL ID | 12047710 |
| MeSH ID | M0277674 |
Synonyms (31)
| Synonym |
|---|
| unii-200ha2limk |
| 200ha2limk , |
| 9,12-epoxy-1h-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-i)(1,6)benzodiazocine-10-carboxylic acid, 5,16-bis((ethylthio)methyl)-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, (9s-(9alpha,10beta,12alpha))- |
| kt 7515 |
| kt-7515 |
| bdbm24942 |
| cep1347 |
| chembl290352 , |
| 3,9-bis(etsm)-k-252a |
| kt7515 |
| 3,9-bis((ethylthio)methyl)-k-252a |
| cep 1347 |
| methyl (15s,16r,18r)-10,23-bis[(ethylsulfanyl)methyl]-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxylate |
| 156177-65-0 |
| cep-1347 |
| kt-1575 |
| gtpl8173 |
| SCHEMBL12047710 |
| (9s,10r,12r)-5-16-bis[(ethylthio)methyl]-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1h-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester |
| AKOS024458422 |
| 9,12-epoxy-1h-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-i)(1,6)benzodiazocine-10-carboxylic acid, 5,16-bis((ethylthio)methyl)-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, (9s-(9.alpha.,10.beta.,12.alpha.))- |
| 9,12-epoxy-1h-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-i)(1,6)benzodiazocine-10-carboxylic acid, 5,16-bis((ethylthio)methyl)-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, (9s,10r,12r)- |
| cep-1374 |
| kt7515;kt-7515;kt 7515;cep-1347;cep 1347 |
| BCP16748 |
| Q27075851 |
| methyl (15s,16r,18r)-10,23-bis(ethylsulfanylmethyl)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8(13),9,11,20(25),21,23,26-nonaene-16-carboxylate |
| MS-30740 |
| methyl (5s,6r,8r)-2,11-bis((ethylthio)methyl)-6-hydroxy-5-methyl-13-oxo-5,6,7,8,14,15-hexahydro-13h-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-6-carboxylate |
| HY-10412 |
| CS-0002594 |
Research Excerpts
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| " Furthermore, expression of wild type MLK3 in hippocampal pyramidal neurons enhanced gp120IIIB-induced neurotoxicity, whereas expression of a dominant negative MLK3 protected neurons from the toxic effects of the glycoprotein." | ( Mixed lineage kinase 3 mediates gp120IIIB-induced neurotoxicity. Bodner, A; Finn, JP; Ghadge, G; Maroney, AC; Miller, RJ; Roos, R, 2002) | 0.31 |
| " In this short-term study, CEP-1347 was safe and well tolerated." | ( The safety and tolerability of a mixed lineage kinase inhibitor (CEP-1347) in PD. , 2004) | 0.32 |
| "The HIV-1 gene products Tat and gp120 are toxic to neurons and can activate cells of myeloid origin, properties that are thought to contribute to the clinical manifestations of HIV-1-associated dementia (HAD)." | ( Inhibition of mixed lineage kinase 3 prevents HIV-1 Tat-mediated neurotoxicity and monocyte activation. Dewhurst, S; Fan, S; Gelbard, HA; Litzburg, A; Maggirwar, SB; Reisinger, E; Schifitto, G; Sniderhan, L; Sui, Z, 2006) | 0.33 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| " We report here URMC-099 (1) an orally bioavailable (F = 41%), potent (IC50 = 14 nM) MLK3 inhibitor with excellent brain exposure in mouse PK models and minimal interference with key human CYP450 enzymes or hERG channels." | ( Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. Dewhurst, S; Gelbard, HA; Goodfellow, VS; Loweth, CJ; Marker, DF; Nguyen, T; Polesskaya, O; Pollack, S; Ravula, SB; Sheppard, D; Todd, DE; Wiemann, T; Xu, Y, 2013) | 0.39 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (8)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| High affinity nerve growth factor receptor | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0002 | 0.5436 | 10.0000 | AID213419 |
| Vascular endothelial growth factor receptor 1 | Homo sapiens (human) | IC50 (µMol) | 0.2090 | 0.0001 | 0.2914 | 7.0000 | AID363165 |
| Vascular endothelial growth factor receptor 3 | Homo sapiens (human) | IC50 (µMol) | 0.0390 | 0.0001 | 0.2264 | 4.9000 | AID363167 |
| Vascular endothelial growth factor receptor 2 | Homo sapiens (human) | IC50 (µMol) | 0.0430 | 0.0000 | 0.4830 | 8.8000 | AID363166 |
| Mitogen-activated protein kinase kinase kinase 9 | Homo sapiens (human) | IC50 (µMol) | 0.0413 | 0.0005 | 0.2244 | 2.1000 | AID125159; AID1384625; AID1798485; AID362969; AID363158; AID775350 |
| Protein delta homolog 1 | Homo sapiens (human) | IC50 (µMol) | 0.1140 | 0.1140 | 0.1260 | 0.1500 | AID1384628; AID363160 |
| Mitogen-activated protein kinase kinase kinase 10 | Homo sapiens (human) | IC50 (µMol) | 0.0412 | 0.0020 | 0.1035 | 0.5800 | AID125160; AID1384626; AID1798485; AID775351 |
| Mitogen-activated protein kinase kinase kinase 11 | Homo sapiens (human) | IC50 (µMol) | 0.0364 | 0.0040 | 0.1021 | 1.1400 | AID125162; AID1384627; AID1798485; AID362970; AID775352 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (130)
Molecular Functions (36)
Ceullar Components (33)
Bioassays (58)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID363167 | Inhibition of human VEGFR3 expressed in baculovirus insect cell system | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. |
| AID1384625 | Inhibition of recombinant GST-tagged human MLK1 KD (1 to 500 residues) expressed in baculovirus using myelin basic protein as substrate preincubated for 15 mins measured after 30 mins in presence of [gamma-32P]ATP by scintillation counting | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration. |
| AID775385 | Inhibition of human wild type FLT3 at 1 uM by qPCR analysis relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID165115 | Inhibition of protein kinase C (PKC) from rat brain homogenate | 2002 | Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2 | Mixed lineage kinase activity of indolocarbazole analogues. |
| AID775458 | Drug uptake in C57BL/6 mouse brain at 10 mg/kg, iv measured at 30 mins | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775372 | Inhibition of human wild type LRRK2 at 1 uM by qPCR analysis relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775349 | Inhibition of human wild type CAMK1D at 1 uM by qPCR analysis relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775330 | Inhibition of wild type human CAMK at 1 uM by qPCR analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775343 | Inhibition of human wild type CAMK2D at 1 uM by qPCR analysis relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775339 | Inhibition of human wild type RSK4 at 1 uM by qPCR analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775450 | Ratio of drug level in brain to plasma in C57BL/6 mouse at 10 mg/kg, iv measured at 180 mins | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775347 | Inhibition of human wild type Aurora kinase A at 1 uM by qPCR analysis relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID363166 | Inhibition of human VEGFR2 expressed in baculovirus insect cell system | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. |
| AID775335 | Inhibition of human ABL1 mutant at 1 uM by qPCR analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775350 | Inhibition of MLK1 (unknown origin) after 20 mins in presence of [33P]-ATP | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID363160 | Inhibition of human DLK expressed in baculovirus insect cell system | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. |
| AID775337 | Binding affinity to human MLK3 | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775369 | Inhibition of human LRRK2 G2019S mutant at 1 uM by qPCR analysis relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID125160 | Inhibition of Mixed lineage kinase 2(MLK2) | 2002 | Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2 | Mixed lineage kinase activity of indolocarbazole analogues. |
| AID775453 | Plasma concentration in C57BL/6 mouse at 10 mg/kg, iv measured at 180 mins | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID363158 | Inhibition of GST-fused human MLK1 expressed in CHO cells assessed as MKK4 phosphorylation | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. |
| AID213419 | Inhibition of NGF high affinity receptor tyrosine kinase TrkA | 2002 | Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2 | Mixed lineage kinase activity of indolocarbazole analogues. |
| AID363196 | Neuroprotective activity against human SH-SY5Y cells assessed as inhibition of MPP+-induced cell death | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. |
| AID775328 | Inhibition of human wild type ABL1 at 1 uM by qPCR analysis relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775341 | Inhibition of human wild type RSK1 at 1 uM by qPCR analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775329 | Inhibition of wild type human AGC kinase at 1 uM by qPCR analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775452 | Ratio of drug level in brain to plasma in C57BL/6 mouse at 10 mg/kg, iv measured at 30 mins | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID1384628 | Inhibition of DLK (unknown origin) using myelin basic protein as substrate preincubated for 15 mins measured after 30 mins in presence of [gamma-32P]ATP by scintillation counting | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration. |
| AID775346 | Inhibition of human wild type Aurora kinase C at 1 uM by qPCR analysis relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775338 | Binding affinity to human wild type TNIK at 1 uM by qPCR analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID362969 | Inhibition of GST-fused human MLK1 | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. |
| AID775454 | Drug uptake in C57BL/6 mouse brain at 10 mg/kg, iv measured at 180 mins | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775344 | Inhibition of human wild type BRSK2 at 1 uM by qPCR analysis relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775455 | Drug uptake in C57BL/6 mouse brain at 10 mg/kg, iv measured at 60 mins | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775348 | Inhibition of human wild type MLK1 at 1 uM by qPCR analysis relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775384 | Inhibition of human wild type KIT at 1 uM by qPCR analysis relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID1384626 | Inhibition of recombinant GST-tagged full length human MLK2 KD/LZ expressed in baculovirus using myelin basic protein as substrate preincubated for 15 mins measured after 30 mins in presence of [gamma-32P]ATP by scintillation counting | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration. |
| AID775345 | Inhibition of human wild type CAMK2A at 1 uM by qPCR analysis relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775352 | Inhibition of MLK3 (unknown origin) after 20 mins in presence of [33P]-ATP | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID363165 | Inhibition of human VEGFR1 expressed in baculovirus insect cell system | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. |
| AID775340 | Binding affinity to human wild type MAP4K4 at 1 uM by qPCR analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775457 | Plasma concentration in C57BL/6 mouse at 10 mg/kg, iv measured at 30 mins | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID363199 | Inhibition of MPTP-induced increase in pMKK4 levels in mouse at 1 mg/kg, po administered 2 hrs before MPTP challenge followed by 10 mg/kg, sc 2 hrs after MPTP challenge | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. |
| AID1384627 | Inhibition of recombinant GST-tagged full length human MLK3 KD expressed in baculovirus using myelin basic protein as substrate preincubated for 15 mins measured after 30 mins in presence of [gamma-32P]ATP by scintillation counting | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration. |
| AID362970 | Inhibition of GST-fused human MLK3 | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. |
| AID775451 | Ratio of drug level in brain to plasma in C57BL/6 mouse at 10 mg/kg, iv measured at 60 mins | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775342 | Inhibition of human wild type AMPKalpha2 at 1 uM by qPCR analysis relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID775456 | Plasma concentration in C57BL/6 mouse at 10 mg/kg, iv measured at 60 mins | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID125159 | Inhibition of Mixed lineage kinase 1 (MLK1) | 2002 | Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2 | Mixed lineage kinase activity of indolocarbazole analogues. |
| AID125162 | Inhibition of Mixed lineage kinase 3 (MLK3) | 2002 | Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2 | Mixed lineage kinase activity of indolocarbazole analogues. |
| AID775351 | Inhibition of MLK2 (unknown origin) after 20 mins in presence of [33P]-ATP | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID1345776 | Human mitogen-activated protein kinase kinase kinase 10 (MLK subfamily) | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID1345760 | Human mitogen-activated protein kinase kinase kinase 9 (MLK subfamily) | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID1345784 | Human mitogen-activated protein kinase kinase kinase 11 (MLK subfamily) | 2001 | The Journal of biological chemistry, Jul-06, Volume: 276, Issue:27 | Cep-1347 (KT7515), a semisynthetic inhibitor of the mixed lineage kinase family. |
| AID1345760 | Human mitogen-activated protein kinase kinase kinase 9 (MLK subfamily) | 2001 | The Journal of biological chemistry, Jul-06, Volume: 276, Issue:27 | Cep-1347 (KT7515), a semisynthetic inhibitor of the mixed lineage kinase family. |
| AID1345784 | Human mitogen-activated protein kinase kinase kinase 11 (MLK subfamily) | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. |
| AID1345776 | Human mitogen-activated protein kinase kinase kinase 10 (MLK subfamily) | 2001 | The Journal of biological chemistry, Jul-06, Volume: 276, Issue:27 | Cep-1347 (KT7515), a semisynthetic inhibitor of the mixed lineage kinase family. |
| AID1798485 | Mixed-Lineage Kinase Assay from Article 10.1021/jm8005838: \\Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo ac | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (72)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 6 (8.33) | 18.2507 |
| 2000's | 54 (75.00) | 29.6817 |
| 2010's | 10 (13.89) | 24.3611 |
| 2020's | 2 (2.78) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 10.47
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 weak demand-to-supply ratio for research on this compound.
| This Compound (10.47) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 4 (5.48%) | 5.53% |
| Reviews | 12 (16.44%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 57 (78.08%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||