| ID Source | ID |
|---|---|
| PubMed CID | 10340781 |
| CHEMBL ID | 228192 |
| SCHEMBL ID | 2387000 |
| MeSH ID | M0540984 |
| Synonym |
|---|
| bdbm50197554 |
| 4-(benzylamino)-2-{[2-(3-chloro-4-hydroxyphenyl)ethyl]amino}pyrimidine-5-carboxamide |
| 2-(3-chloro-4-hydroxyphenethylamino)-4-(benzylamino)pyrimidine-5-carboxamide |
| as-1517499 |
| CHEMBL228192 , |
| AKOS016013167 |
| as1517499 |
| 919486-40-1 |
| S8685 |
| 5-pyrimidinecarboxamide, 2-((2-(3-chloro-4-hydroxyphenyl)ethyl)amino)-4-((phenylmethyl)amino)- |
| 2h31hot08t , |
| as-1571499 |
| unii-2h31hot08t |
| 4-(benzylamino)-2-((3-chloro-4-hydroxyphenethyl)amino)pyrimidine-5-carboxamide |
| OZRMEKAUZBKTTC-UHFFFAOYSA-N , |
| 4-benzylamino-2-{[2-(3-chloro-4-hydroxyphenyl)ethyl]amino}pyrimidine-5-carboxamide |
| SCHEMBL2387000 |
| as 1517499 |
| 4-(benzylamino)-2-(3-chloro-4-hydroxyphenethylamino)pyrimidine-5-carboxamide |
| CS-6099 |
| HY-100614 |
| DTXSID30238798 |
| AS-73883 |
| NCGC00386673-01 |
| as1517499, >=98% (hplc) |
| EX-A2470 |
| as-1517499; as 1517499 |
| BCP13796 |
| 4-(benzylamino)-2-[2-(3-chloro-4-hydroxyphenyl)ethylamino]pyrimidine-5-carboxamide |
| HMS3740O03 |
| CCG-268628 |
| C77148 |
| Q27254731 |
| A916321 |
| SB55495 |
| AC-35726 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " To search for potent and orally bioavailable STAT6 inhibitors, we synthesized a series of 4-benzylaminopyrimidine-5-carboxamide derivatives and evaluated their STAT6 inhibitory activities." | ( Identification of 4-benzylamino-2-[(4-morpholin-4-ylphenyl)amino]pyrimidine-5-carboxamide derivatives as potent and orally bioavailable STAT6 inhibitors. Iwata, M; Koakutsu, A; Kuromitsu, S; Moritomo, H; Nagashima, S; Nagata, H; Ohga, K; Ohta, M; Orita, M; Takeuchi, M; Tsukamoto, S; Yokota, M, 2008) | 0.35 |
| "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 (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 6.0081 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 6.7412 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 15.0916 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 6.7412 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 6.7412 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 6.7412 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 6.7412 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [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) |
|---|---|---|---|---|---|---|---|
| Signal transducer and activator of transcription 6 | Homo sapiens (human) | IC50 (µMol) | 0.0210 | 0.0210 | 0.0210 | 0.0210 | AID284275; AID343057 |
| Rho-associated protein kinase 2 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0210 | 0.0210 | 3.0652 | 7.7000 | AID284275 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID284277 | Effect on differentiation of C57BL/6 mouse T cells assessed as inhibition of IL12-induced TFN-gamma production | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2 | Synthesis and evaluation of 2-{[2-(4-hydroxyphenyl)-ethyl]amino}pyrimidine-5-carboxamide derivatives as novel STAT6 inhibitors. |
| AID284275 | Inhibition of STAT6 in human IL4-stimulated FW4 cells | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2 | Synthesis and evaluation of 2-{[2-(4-hydroxyphenyl)-ethyl]amino}pyrimidine-5-carboxamide derivatives as novel STAT6 inhibitors. |
| AID343057 | Inhibition of STAT6 activation in FW4 reporter cells | 2008 | Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13 | Identification of 4-benzylamino-2-[(4-morpholin-4-ylphenyl)amino]pyrimidine-5-carboxamide derivatives as potent and orally bioavailable STAT6 inhibitors. |
| AID284278 | Effect on differentiation of C57BL/6 mouse T cells assessed as inhibition of IL4 production | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2 | Synthesis and evaluation of 2-{[2-(4-hydroxyphenyl)-ethyl]amino}pyrimidine-5-carboxamide derivatives as novel STAT6 inhibitors. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 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. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| 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. |
| 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. |
| 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. |
| [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 | 2 (40.00) | 29.6817 |
| 2010's | 1 (20.00) | 24.3611 |
| 2020's | 2 (40.00) | 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 (12.84) 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] | ||