JNJ-40346527: inhibits colony-stimulating factor-1 receptor kinase [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 25230468 |
| CHEMBL ID | 3674570 |
| SCHEMBL ID | 4238665 |
| SCHEMBL ID | 21396445 |
| MeSH ID | M000613767 |
| Synonym |
|---|
| us8497376, 15 |
| bdbm98634 |
| SCHEMBL4238665 |
| AC-33642 |
| CHEMBL3674570 |
| edicotinibjnj-40346527 |
| edicotinib [inn] |
| edicotinib [who-dd] |
| edicotinib |
| 4-cyano-n-[2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyloxan-4-yl)pyridin-3-yl]-1h-imidazole-2-carboxamide |
| jnj-40346527 |
| jnj40346527 |
| gtpl8942 |
| 1h-imidazole-2-carboxamide, 5-cyano-n-(2-(4,4-dimethyl-1-cyclohexen-1-yl)-6-(tetrahydro-2,2,6,6-tetramethyl-2h-pyran-4-yl)-3-pyridinyl)- |
| edicotinib [usan] |
| unii-3nu609vynf |
| 1142363-52-7 |
| 4-cyano-n-(2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyl-tetrahydro-2h-pyran-4-yl)pyridin-3-yl)-1h-imidazole-2-carboxamide |
| 4-cyano-1h-imidazole-2-carboxylic acid n-(2-(4,4-dimethylcyclohex-1-enyl)-6-(2,2,6,6-tetramethyltetrahydropyran-4-yl)pyridin-3-yl)amide |
| 3NU609VYNF , |
| AKOS030527728 |
| bdbm276743 |
| us10071991, compound (p) |
| DB12504 |
| 4-cyano-n-(2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2h-pyran-4-yl)pyridin-3-yl)-1h-imidazole-2-carboxamide |
| BCP25086 |
| HY-109086 |
| CS-0039264 |
| Q27893923 |
| BS-14512 |
| 5-cyano-n-(2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2h-pyran-4-yl)pyridin-3-yl)-1h-imidazole-2-carboxamide |
| BNVPFDRNGHMRJS-UHFFFAOYSA-N , |
| 4-cyano-1h-imidazole-2-carboxylic acid[2-(4,4-dimethyl-cyclohex-1-enyl)-6-(2,2,6,6-tetramethyl-tetrahydro-pyran-4-yl)-pyridin-3-yl]-amide |
| D11378 |
| edicotinib (usan) |
| EX-A2787 |
| jnj-527jnj-40346527 |
| jnj-527 |
| 5-cyano-n-[2-(4,4-dimethylcyclohexen-1-yl)-6-(2,2,6,6-tetramethyloxan-4-yl)pyridin-3-yl]-1h-imidazole-2-carboxamide |
| D83692 |
| SCHEMBL21396445 |
| A930079 |
| 4-cyano-n-(2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2h-pyran-4-yl)pyridin-3-yl)- 1h-imidazole-2-carboxamide |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) | IC50 (µMol) | 0.0032 | 0.0006 | 0.5676 | 5.5450 | AID1388781; AID1757450 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| protein tyrosine kinase activity | Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) |
| macrophage colony-stimulating factor receptor activity | Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) |
| protein binding | Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) |
| ATP binding | Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) |
| protein phosphatase binding | Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) |
| cytokine binding | Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) |
| protein homodimerization activity | Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) |
| growth factor binding | Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| nucleoplasm | Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) |
| plasma membrane | Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) |
| cell surface | Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) |
| intracellular membrane-bounded organelle | Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) |
| CSF1-CSF1R complex | Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) |
| receptor complex | Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) |
| plasma membrane | Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1388784 | In vivo inhibition of CSF1R phosphorylation in cHL patient at 150 mg administered daily as multiple dose | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors. |
| AID1757450 | Inhibition of CSF1R (unknown origin) (538 to 972 residues) expressed in baculovirus expression system using SYEGNSYTFIDPTQ as substrate incubated for 80 mins in presence of ATP by fluorescence polarization assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Discovery of potent colony-stimulating factor 1 receptor inhibitors by replacement of hinge-binder moieties. |
| AID1388783 | In vivo inhibition of CSF1R phosphorylation in cHL patient at 450 mg administered as single dose | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors. |
| AID1388781 | Inhibition of CSF1R (unknown origin) | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors. |
| AID1388782 | Tmax in cHL patient at 10 mg administered as single dose | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors. |
| AID1345503 | Human fms related tyrosine kinase 3 (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2015 | The Journal of rheumatology, Oct, Volume: 42, Issue:10 | Results from a Phase IIA Parallel Group Study of JNJ-40346527, an Oral CSF-1R Inhibitor, in Patients with Active Rheumatoid Arthritis despite Disease-modifying Antirheumatic Drug Therapy. |
| AID1345555 | Human KIT proto-oncogene receptor tyrosine kinase (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2015 | The Journal of rheumatology, Oct, Volume: 42, Issue:10 | Results from a Phase IIA Parallel Group Study of JNJ-40346527, an Oral CSF-1R Inhibitor, in Patients with Active Rheumatoid Arthritis despite Disease-modifying Antirheumatic Drug Therapy. |
| AID1345508 | Human colony stimulating factor 1 receptor (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2015 | The Journal of rheumatology, Oct, Volume: 42, Issue:10 | Results from a Phase IIA Parallel Group Study of JNJ-40346527, an Oral CSF-1R Inhibitor, in Patients with Active Rheumatoid Arthritis despite Disease-modifying Antirheumatic Drug Therapy. |
| [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 | 8 (88.89) | 24.3611 |
| 2020's | 1 (11.11) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (21.36) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 2 (22.22%) | 5.53% |
| Reviews | 2 (22.22%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (55.56%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||