Assay Detail
Binding
CHEMBL2330282
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Inhibition of PRMT3 (unknown origin) using histone H4 (1 to 24) as substrate after 1 hr by scintillation proximity assay in presence of [3H]-S-adenosylmethionine
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Protein arginine N-methyltransferase 3 (CHEMBL5891) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Exploiting an allosteric binding site of PRMT3 yields potent and selective inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 47 | 5.72 | 6.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2325198 | — | — | 1 | 6.64 |
| CHEMBL2325177 | — | — | 1 | 6.52 |
| CHEMBL2325197 | — | — | 1 | 6.44 |
| CHEMBL2325183 | — | — | 1 | 6.32 |
| CHEMBL2325195 | — | — | 1 | 6.31 |
| CHEMBL2325196 | — | — | 1 | 6.08 |
| CHEMBL2325178 | — | — | 1 | 6.07 |
| CHEMBL2325442 | — | — | 1 | 6.00 |
| CHEMBL2325179 | — | — | 1 | 5.75 |
| CHEMBL2325191 | — | — | 1 | 5.72 |
| CHEMBL2325184 | — | — | 1 | 5.66 |
| CHEMBL2325441 | — | — | 1 | 5.62 |
| CHEMBL2325185 | — | — | 1 | 5.57 |
| CHEMBL2325180 | — | — | 1 | 5.51 |
| CHEMBL2325189 | — | — | 1 | 5.48 |
| CHEMBL2325194 | — | — | 1 | 5.48 |
| CHEMBL2325186 | — | — | 1 | 5.44 |
| CHEMBL2325163 | — | — | 1 | 5.44 |
| CHEMBL2325181 | — | — | 1 | 5.40 |
| CHEMBL2325193 | — | — | 1 | 5.36 |
| CHEMBL2325192 | — | — | 1 | 5.30 |
| CHEMBL2325188 | — | — | 1 | 5.28 |
| CHEMBL2325164 | — | — | 1 | 5.28 |
| CHEMBL2325190 | — | — | 1 | 5.23 |
| CHEMBL2325166 | — | — | 1 | 5.14 |
| CHEMBL2325443 | — | — | 1 | - |
| CHEMBL2325444 | — | — | 1 | - |
| CHEMBL2325445 | — | — | 1 | - |
| CHEMBL2325446 | — | — | 1 | - |
| CHEMBL2325447 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2325198 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2325177 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2325197 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL2325183 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL2325195 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL2325196 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL2325178 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL2325442 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2325179 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL2325191 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2325184 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2325441 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2325185 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL2325180 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL2325194 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL2325189 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL2325186 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL2325163 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL2325181 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2325193 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL2325192 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2325188 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL2325164 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL2325190 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL2325166 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL2325182 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL2325176 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2325175 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL2325174 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2325173 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL2325172 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL2325171 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL2325170 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2325169 | — | IC50 | > | 15000.0 | nM | - |
| CHEMBL2325168 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2325167 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2325165 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2325187 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2325162 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2325161 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2325160 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2325448 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2325447 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2325446 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2325445 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2325444 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2325443 | — | IC50 | > | 100000.0 | nM | - |