Assay Detail
Binding
CHEMBL1908798
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Binding constant for TAOK3 kinase domain
72
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase TAO3 (CHEMBL5701) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 6.40 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 9.66 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 8.24 |
| CHEMBL450786 | PHA-665752 | — | 1 | 7.37 |
| CHEMBL509032 | TAE-684 | — | 1 | 7.36 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 7.35 |
| CHEMBL445813 | AT-7519 | 2.0 | 1 | 7.24 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 7.09 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.07 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 7.01 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 7.00 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.68 |
| CHEMBL384304 | RG-547 | 2.0 | 1 | 6.68 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 6.58 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 6.51 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 6.47 |
| CHEMBL386051 | — | — | 1 | 6.41 |
| CHEMBL1241674 | — | — | 1 | 6.31 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.31 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 6.23 |
| CHEMBL296468 | BMS-387032 | 1.0 | 1 | 6.21 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | 6.14 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.00 |
| CHEMBL379218 | — | — | 1 | 5.96 |
| CHEMBL464552 | — | — | 1 | 5.85 |
| CHEMBL1908394 | GSK-461364 | 1.0 | 1 | 5.85 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 5.77 |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 5.77 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 5.72 |
| CHEMBL1908395 | — | — | 1 | 5.66 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | Kd | = | 0.22 | nM | 9.66 |
| CHEMBL574738 | AST-487 | Kd | = | 5.8 | nM | 8.24 |
| CHEMBL450786 | PHA-665752 | Kd | = | 43.0 | nM | 7.37 |
| CHEMBL509032 | TAE-684 | Kd | = | 44.0 | nM | 7.36 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 45.0 | nM | 7.35 |
| CHEMBL445813 | AT-7519 | Kd | = | 57.0 | nM | 7.24 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 81.0 | nM | 7.09 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 86.0 | nM | 7.07 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 97.0 | nM | 7.01 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 99.0 | nM | 7.00 |
| CHEMBL535 | SUNITINIB | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL384304 | RG-547 | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL223360 | LINIFANIB | Kd | = | 260.0 | nM | 6.58 |
| CHEMBL1721885 | SU-014813 | Kd | = | 310.0 | nM | 6.51 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 340.0 | nM | 6.47 |
| CHEMBL386051 | — | Kd | = | 390.0 | nM | 6.41 |
| CHEMBL1241674 | — | Kd | = | 490.0 | nM | 6.31 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 490.0 | nM | 6.31 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 590.0 | nM | 6.23 |
| CHEMBL296468 | BMS-387032 | Kd | = | 620.0 | nM | 6.21 |
| CHEMBL558752 | RAF-265 | Kd | = | 720.0 | nM | 6.14 |
| CHEMBL1908397 | KW-2449 | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL379218 | — | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL464552 | — | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL255863 | NILOTINIB | Kd | = | 1700.0 | nM | 5.77 |
| CHEMBL513909 | BI-2536 | Kd | = | 1700.0 | nM | 5.77 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL1908395 | — | Kd | = | 2200.0 | nM | 5.66 |
| CHEMBL5416410 | DASATINIB | Kd | = | 2300.0 | nM | 5.64 |
| CHEMBL230011 | TG100-115 | Kd | = | 2400.0 | nM | 5.62 |
| CHEMBL1336 | SORAFENIB | Kd | = | 2700.0 | nM | 5.57 |
| CHEMBL180022 | NERATINIB | Kd | = | 4200.0 | nM | 5.38 |
| CHEMBL475251 | R-406 | Kd | = | 4600.0 | nM | 5.34 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 5000.0 | nM | 5.30 |
| CHEMBL494089 | GSK-690693 | Kd | = | 9300.0 | nM | 5.03 |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL31965 | CANERTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1173655 | AFATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL573339 | PI-103 | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL502835 | NINTEDANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL1908396 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 10000.0 | nM | - |