| ID Source | ID |
|---|---|
| PubMed CID | 16095343 |
| CHEMBL ID | 1956071 |
| SCHEMBL ID | 15799497 |
| MeSH ID | M0506510 |
| Synonym |
|---|
| bdbm50365218 |
| sb-772077b |
| sb-7720770b |
| CHEMBL1956071 , |
| AB01092286-01 |
| SCHEMBL15799497 |
| NCGC00241969-05 |
| nsc756491 |
| nsc-756491 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Inhibitor of nuclear factor kappa-B kinase subunit beta | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0009 | 0.9781 | 9.8200 | AID649977 |
| Rho-associated protein kinase 2 | Homo sapiens (human) | IC50 (µMol) | 0.0065 | 0.0002 | 0.5780 | 10.0000 | AID1165785; AID649969 |
| Ribosomal protein S6 kinase alpha-5 | Homo sapiens (human) | IC50 (µMol) | 0.0140 | 0.0004 | 1.3066 | 8.3000 | AID649971 |
| Cyclin-dependent kinase 2 | Homo sapiens (human) | IC50 (µMol) | 7.0000 | 0.0004 | 1.0444 | 10.0000 | AID649975 |
| RAC-alpha serine/threonine-protein kinase | Homo sapiens (human) | IC50 (µMol) | 0.3240 | 0.0002 | 0.7387 | 10.0000 | AID649972 |
| RAC-beta serine/threonine-protein kinase | Homo sapiens (human) | IC50 (µMol) | 1.9500 | 0.0005 | 0.5013 | 7.6000 | AID649973 |
| Glycogen synthase kinase-3 alpha | Homo sapiens (human) | IC50 (µMol) | 9.1000 | 0.0010 | 1.2249 | 9.1000 | AID649976 |
| Serine/threonine-protein kinase PLK1 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0001 | 0.7734 | 9.0000 | AID650110 |
| Mitogen-activated protein kinase 10 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0020 | 1.7035 | 10.0000 | AID650109 |
| Rho-associated protein kinase 1 | Homo sapiens (human) | IC50 (µMol) | 0.0084 | 0.0004 | 0.8549 | 10.0000 | AID1165784; AID1564132; AID649968 |
| Ribosomal protein S6 kinase alpha-1 | Homo sapiens (human) | IC50 (µMol) | 0.0350 | 0.0001 | 0.1861 | 1.2600 | AID649970 |
| Serine/threonine-protein kinase TBK1 | Homo sapiens (human) | IC50 (µMol) | 1.6400 | 0.0022 | 0.8565 | 6.2200 | AID1801133 |
| RAC-gamma serine/threonine-protein kinase | Homo sapiens (human) | IC50 (µMol) | 1.2900 | 0.0006 | 0.4743 | 4.0000 | AID649974 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID650110 | Inhibition of PLK | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID650124 | Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL-6 production treated 30 mins before LPS stimulation measured after 18 hrs by ELISA | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID650131 | Antihypertensive activity in rat assessed as reduction of DOCA salt-induced blood pressure at 1 mg/kg, po after 2 hrs | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID650129 | Antihypertensive activity in spontaneously hypertensive rat assessed as reduction of blood pressure at 0.3 to 3 mg/kg, po after 2 hrs | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID649976 | Inhibition of GSK3alpha | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID649969 | Inhibition of human ROCK2 | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID1165784 | Inhibition of ROCK-1 (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension. |
| AID649973 | Inhibition of AKT2 | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID1165795 | Toxicity in Lewis rat at 30 mg/kg, po administered as single dose measured after 1 to 24 hrs | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension. |
| AID1165789 | Selectivity ratio of IC50 for protein kinase A (unknown origin) to IC50 for ROCK (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension. |
| AID650109 | Inhibition of JNK3 | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID650127 | Vasodilatory activity in Sprague-Dawley rat aorta assessed as reversal of KCl/phenylephrine-induced muscle contraction | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID649968 | Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID649977 | Inhibition of IKK2 | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID650123 | Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production treated 30 mins before LPS stimulation measured after 18 hrs by ELISA | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID649972 | Inhibition of AKT1 | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID649971 | Inhibition of MSK1 | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID1165785 | Inhibition of human recombinant ROCK-2 using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK as substrate after 40 mins by scintillation counting analysis | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension. |
| AID650121 | Inhibition of angiotensin-2-induced actin stress fiber formation in human primary aortic smooth muscle cells at 1 uM treated 30 mins before angiotensin-2 stimulation measured after 2 hrs using rhodamine phalloidin staining by confocal microscopic analysis | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID649975 | Inhibition of CDK2 | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID649967 | Antihypertensive activity in po dosed spontaneously hypertensive rat assessed as reduction of blood pressure | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID650130 | Cardiovascular activity in spontaneously hypertensive rat assessed as increase in heart rate at 0.3 to 3 mg/kg, po | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID650133 | Cardiovascular activity in DOCA salt treated rat assessed as increase in heart rate at 1 mg/kg, po | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID650132 | Antihypertensive activity in spontaneously hypertensive rat assessed as reduction of blood pressure at 1 mg/kg, po after 2 hrs | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID649974 | Inhibition of AKT3 | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID650134 | Antihypertensive activity in normotensive Sprague-Dawley rat assessed as reduction of blood pressure at 1 mg/kg, po after 2 hrs | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID1564132 | Inhibition of N-terminal His-tagged human ROCK1 (3 to 543 residues) expressed in baculovirus infected Sf9 cells using biotin-Ahx-AKRRRLSSLRA-CONH2 as substrate incubated for 90 mins in presence of [gamma33P]ATP by scintillation counting method | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Potently inhibiting cancer cell migration with novel 3H-pyrazolo[4,3-f]quinoline boronic acid ROCK inhibitors. |
| AID649970 | Inhibition of RSK1 | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID650128 | Vasodilatory activity in Sprague-Dawley rat aorta assessed as reversal of KCl/phenylephrine-induced muscle contraction measured after drug washout | 2007 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 320, Issue:1 | Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. |
| AID1165796 | Reduction of peripheral lymphocyte count in Lewis rat at 30 mg/kg, po | 2014 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20 | Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension. |
| AID1801133 | KinEASE-STK Assay from Article 10.1021/cb500908d: \\Identification and further development of potent TBK1 inhibitors.\\ | 2015 | ACS chemical biology, Jan-16, Volume: 10, Issue:1 | Identification and further development of potent TBK1 inhibitors. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (20.00) | 29.6817 |
| 2010's | 4 (80.00) | 24.3611 |
| 2020's | 0 (0.00) | 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 weak demand-to-supply ratio for research on this compound.
| This Compound (13.28) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||