Assay Detail
Binding
CHEMBL3991891
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
234
Total Activities
234
Compounds Tested
1
Activity Types
1
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | K-562, COLO 205, SK-N-BE(2) and MV-4-11 |
| Subcellular | Cell lysate |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase STK11 (CHEMBL5606) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 234 | 6.34 | 8.52 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 8.52 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 6.36 |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | 6.30 |
| CHEMBL1084546 | PF-00562271 | 1.0 | 1 | 6.20 |
| CHEMBL1231124 | AZD-1480 | 2.0 | 1 | 6.15 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 5.51 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 5.36 |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | - |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | - |
| CHEMBL2079588 | TELATINIB | 2.0 | 1 | - |
| CHEMBL3186534 | RIVOCERANIB | 3.0 | 1 | - |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | - |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | - |
| CHEMBL536151 | IMD-0354 | 1.0 | 1 | - |
| CHEMBL281948 | K-252A | — | 1 | - |
| CHEMBL14762 | SELICICLIB | 2.0 | 1 | - |
| CHEMBL3991935 | — | — | 1 | - |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | - |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | - |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | - |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | - |
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | - |
| CHEMBL571948 | Y-39983 | 1.0 | 1 | - |
| CHEMBL488436 | AZD-5438 | 1.0 | 1 | - |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | - |
| CHEMBL592445 | GEDATOLISIB | 3.0 | 1 | - |
| CHEMBL403989 | TG100-801 | 2.0 | 1 | - |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | - |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | - |
| CHEMBL283120 | AXL-1717 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2035187 | PACRITINIB | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 434.0 | nM | 6.36 |
| CHEMBL2103840 | DINACICLIB | Kd | = | 497.0 | nM | 6.30 |
| CHEMBL1084546 | PF-00562271 | Kd | = | 626.0 | nM | 6.20 |
| CHEMBL1231124 | AZD-1480 | Kd | = | 714.0 | nM | 6.15 |
| CHEMBL3545085 | XL-228 | Kd | = | 3077.0 | nM | 5.51 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 4375.0 | nM | 5.36 |
| CHEMBL1614766 | RO-4987655 | Kd | > | 30000.0 | nM | - |
| CHEMBL1094408 | NMS-1286937 | Kd | > | 30000.0 | nM | - |
| CHEMBL1088751 | PH-797804 | Kd | > | 30000.0 | nM | - |
| CHEMBL1289494 | TIVOZANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3039517 | RABUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | > | 30000.0 | nM | - |
| CHEMBL372764 | PERIFOSINE | Kd | > | 30000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL4289017 | PF-03814735 | Kd | > | 30000.0 | nM | - |
| CHEMBL1615025 | TAK-733 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545083 | RGB-286638 | Kd | > | 30000.0 | nM | - |
| CHEMBL3109738 | JNJ-26483327 | Kd | > | 30000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 30000.0 | nM | - |
| CHEMBL507361 | MIRDAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991927 | HMN-214 | Kd | > | 30000.0 | nM | - |
| CHEMBL1289601 | LENVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | Kd | > | 30000.0 | nM | - |
| CHEMBL288441 | BOSUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544966 | GSK-1059615 | Kd | > | 30000.0 | nM | - |
| CHEMBL2220486 | LUCITANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545076 | LY-2584702 | Kd | > | 30000.0 | nM | - |
| CHEMBL1171837 | PONATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL513909 | BI-2536 | Kd | > | 30000.0 | nM | - |
| CHEMBL2107832 | PIMASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2001019 | PF-04217903 | Kd | > | 30000.0 | nM | - |
| CHEMBL1879463 | DACTOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2216870 | IDELALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL572878 | TOZASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL608533 | MIDOSTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL2103842 | VARLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2146883 | COBIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1241855 | RIGOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3184679 | AZD-4547 | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL384304 | RG-547 | Kd | > | 30000.0 | nM | - |
| CHEMBL1908360 | EVEROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL475251 | R-406 | Kd | > | 30000.0 | nM | - |
| CHEMBL3188267 | CAPMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL274654 | ORANTINIB | Kd | > | 30000.0 | nM | - |