ono-8430506 profile

ONO-8430506: an autotaxin inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	56597976
CHEMBL ID	4649390
SCHEMBL ID	14892670
MeSH ID	M000598707

Synonym
SCHEMBL14892670
ono-8430506
MS-28471
EX-A5185
1354805-08-5
HY-145344
bdbm50542080
CHEMBL4649390 ,
CS-0371631
AKOS040756675

Excerpt	Relevance	Reference
" In this study, we showed that dosing rats with ONO-8430506 decreased intraurethral pressure accompanied by urethral relaxation."	( A novel highly potent autotaxin/ENPP2 inhibitor produces prolonged decreases in plasma lysophosphatidic acid formation in vivo and regulates urethral tension. Hayashi, A; Katoh, M; Kishikawa, K; Komichi, Y; Maeda, T; Matsumura, N; Mizuno, H; Nakade, S; Ohhata, A; Ota, H; Saga, H; Shibaya, M; Sugiyama, T; Takada, Y, 2014)	0.66

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)	IC50 (µMol)	0.0100	0.0011	1.0958	10.0000	AID1658784
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
chemotaxis	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
immune response	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
phospholipid catabolic process	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
positive regulation of epithelial cell migration	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
vesicle-mediated transport	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
sphingolipid catabolic process	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
regulation of cell migration	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
phosphatidylcholine catabolic process	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
cell motility	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
positive regulation of lamellipodium morphogenesis	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
nucleic acid binding	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
lysophospholipase activity	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
scavenger receptor activity	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
calcium ion binding	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
zinc ion binding	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
hydrolase activity	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
polysaccharide binding	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
alkylglycerophosphoethanolamine phosphodiesterase activity	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
phosphodiesterase I activity	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
extracellular space	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
plasma membrane	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
extracellular space	Ectonucleotide pyrophosphatase/phosphodiesterase family member 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (29)

Assay ID	Title	Year	Journal	Article
AID1658802	Volume of distribution at steady state in Sprague-Dawley rat at 0.3 mg/kg, iv administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658808	Half life in Beagle dog at 0.3 mg/kg, iv administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658819	In vivo inhibition of lysoPLD activity of ATX in SCID mouse plasma xenografted with human MDA-MB-231 cells at 100 mg/kg, po administered twice daily for 32 days in combination with paclitaxel at 20 mg/kg, ip three times weekly for 5 weeks and measured at	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658784	Inhibition of recombinant human ATX assessed as reduction in choline release using LPC(16:0) as substrate incubated for 15 hrs	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658813	Oral bioavailability in Beagle dog at 1 mg/kg administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658820	Volume of distribution at steady state in cynomolgus monkey at 0.3 mg/kg, iv administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658792	Protein binding in human plasma measured after 4 hrs by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658814	Oral bioavailability in Sprague-Dawley rat at 1 mg/kg administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658822	Half life in cynomolgus monkey at 0.3 mg/kg, iv administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658804	Half life in Sprague-Dawley rat at 1 mg/kg, po administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658800	Half life in SCID mouse at 1 mg/kg, po administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658812	Oral bioavailability in cynomolgus monkey at 1 mg/kg administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658805	Clearance in Sprague-Dawley rat at 0.3 mg/kg, iv administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658801	Cmax in Sprague-Dawley rat at 1 mg/kg, po administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658810	Clearance in Beagle dog at 0.3 mg/kg, iv administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658799	Cmax in SCID mouse at 1 mg/kg, po administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658803	Half life in Sprague-Dawley rat at 0.3 mg/kg, iv administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658809	Half life in Beagle dog at 1 mg/kg, po administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658818	In vivo inhibition of lysoPLD activity of ATX in SCID mouse plasma xenografted with human MDA-MB-231 cells at 30 mg/kg, po administered twice daily for 32 days in combination with paclitaxel at 20 mg/kg, ip three times weekly for 5 weeks and measured at 1	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658815	Antitumor activity against human MDA-MB-231 cells xenografted in SCID mouse assessed as tumor growth inhibition at 100 mg/kg, po administered twice daily for 32 days and measured on day 33 relative to control	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658816	Potentiation of paclitaxel-induced antitumor activity against human MDA-MB-231 cells xenografted in SCID mouse assessed as tumor growth inhibition at 30 mg/kg, po administered twice daily for 32 days in combination with paclitaxel at 20 mg/kg, ip three ti	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658793	Protein binding in rat plasma measured after 4 hrs by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658806	Cmax in Beagle dog at 1 mg/kg, po administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658823	Clearance in cynomolgus monkey at 0.3 mg/kg, iv administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658817	Potentiation of paclitaxel-induced antitumor activity against human MDA-MB-231 cells xenografted in SCID mouse assessed as tumor growth inhibition at 100 mg/kg, po administered twice daily for 32 days in combination with paclitaxel at 20 mg/kg, ip three t	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658811	Cmax in cynomolgus monkey at 1 mg/kg, po administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658807	Volume of distribution at steady state in Beagle dog at 0.3 mg/kg, iv administered as single dose by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658798	AUC in Sprague-Dawley rat at 0.5 mg/kg, po administered as single cassette dosing by LC-MS/MS analysis	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
AID1658791	Inhibition of LysoPLD activity of ATX in human plasma assessed as reduction in choline release using LPC(16:0) as substrate incubated for 15 hrs	2020	ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6	ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.
[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	0 (0.00)	29.6817
2010's	3 (50.00)	24.3611
2020's	3 (50.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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	6 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
sphingosine sphing-4-enine : A sphingenine in which the C=C double bond is located at the 4-position.. sphingenine : A 2-aminooctadecene-1,3-diol having (2S,3R)-configuration.. sphingoid : Sphinganine, its homologs and stereoisomers, and the hydroxy and unsaturated derivatives of these compounds.. 2-aminooctadec-4-ene-1,3-diol : A 2-aminooctadecene-1,3-diol having its double bond at position 4.	2.11	1	sphing-4-enine	human metabolite; mouse metabolite
sphingosine 1-phosphate sphingosine 1-phosphate: RN given refers to (R-(R,S-(E)))-isomer; RN for cpd without isomeric designation not available 8/89. sphingosine 1-phosphate : A phosphosphingolipid that consists of sphingosine having a phospho group attached at position 1	2.11	1	sphingoid 1-phosphate	mouse metabolite; signalling molecule; sphingosine-1-phosphate receptor agonist; T-cell proliferation inhibitor; vasodilator agent
lysophosphatidic acid lysophosphatidic acid: RN given refers to parent cpd. 1-oleoyl-sn-glycerol 3-phosphate : A 1-acyl-sn-glycerol 3-phosphate having oleoyl as the 1-O-acyl group.. lysophosphatidic acid : A member of the class of lysophosphatidic acids obtained by hydrolytic removal of one of the two acyl groups of any phosphatidic acid. A 'closed' class.	3.04	4	1-acyl-sn-glycerol 3-phosphate
lysophosphatidylcholines lysophosphatidylcholine : An acylglycerophosphocholine resulting from partial hydrolysis of a phosphatidylcholine, which removes one of the fatty acyl groups. The structure is depicted in the image where R1 = acyl, R2 = H or where R1 = H, R2 = acyl.	2.31	1	1-O-acyl-sn-glycero-3-phosphocholine

Condition	Relationship Strength	Studies
Benign Neoplasms [description not available]	2.6	1
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	2.6	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.31	1
Nerve Pain [description not available]	2.31	1
Neuralgia Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.	2.31	1
Spinal Stenosis Narrowing of the spinal canal.	2.31	1
Cancer of Lung [description not available]	2.1	1
Experimental Mammary Neoplasms [description not available]	2.1	1
Lung Neoplasms Tumors or cancer of the LUNG.	2.1	1
Muscle Relaxation That phase of a muscle twitch during which a muscle returns to a resting position.	2.1	1
Innate Inflammatory Response [description not available]	2.11	1
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	2.11	1

ono-8430506

Description

Cross-References

Synonyms (10)

Research Excerpts

Dosage Studied

Protein Targets (1)

Inhibition Measurements

Biological Processes (11)

Molecular Functions (9)

Ceullar Components (2)

Bioassays (29)

Research

Studies (6)

Market Indicators

Research Demand Index: 20.35

Study Types

ono-8430506

Description

Cross-References

Synonyms (10)

Research Excerpts

Dosage Studied

Protein Targets (1)

Inhibition Measurements

Biological Processes (11)

Molecular Functions (9)

Ceullar Components (2)

Bioassays (29)

Research

Studies (6)

Market Indicators

Research Demand Index: 20.35

Study Types

Related Drugs (4)

Related Conditions (12)