Assay Detail
Binding
CHEMBL3266887
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Binding affinity to His-tagged MCL1 (171 to 327) (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as inhibition of MCL1-N-terminal biotin-labeled BIM BH3 peptide interaction after 30 mins by surface plasmon resonance analysis
46
Total Activities
46
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
Induced myeloid leukemia cell differentiation protein Mcl-1 (CHEMBL4361) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
3-Substituted-N-(4-hydroxynaphthalen-1-yl)arylsulfonamides as a novel class of selective Mcl-1 inhibitors: structure-based design, synthesis, SAR, and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 5.14 | 6.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3265297 | — | — | 1 | 6.06 |
| CHEMBL3265300 | — | — | 1 | 6.05 |
| CHEMBL3265298 | — | — | 1 | 6.04 |
| CHEMBL3265299 | — | — | 1 | 5.84 |
| CHEMBL3265313 | — | — | 1 | 5.82 |
| CHEMBL3265294 | — | — | 1 | 5.69 |
| CHEMBL3265295 | — | — | 1 | 5.64 |
| CHEMBL1331211 | — | — | 1 | 5.62 |
| CHEMBL1564699 | — | — | 1 | 5.57 |
| CHEMBL3235895 | — | — | 1 | 5.56 |
| CHEMBL3265310 | — | — | 1 | 5.41 |
| CHEMBL3235886 | — | — | 1 | 5.40 |
| CHEMBL3260033 | — | — | 1 | 5.30 |
| CHEMBL1888104 | — | — | 1 | 5.30 |
| CHEMBL3265292 | — | — | 1 | 5.21 |
| CHEMBL2030270 | — | — | 1 | 5.15 |
| CHEMBL1465938 | — | — | 1 | 5.14 |
| CHEMBL3265293 | — | — | 1 | 5.12 |
| CHEMBL3265290 | — | — | 1 | 5.06 |
| CHEMBL1607263 | — | — | 1 | 5.06 |
| CHEMBL3265303 | — | — | 1 | 5.02 |
| CHEMBL3265291 | — | — | 1 | 5.01 |
| CHEMBL3265296 | — | — | 1 | 5.00 |
| CHEMBL3265311 | — | — | 1 | 4.96 |
| CHEMBL1868007 | — | — | 1 | 4.94 |
| CHEMBL1865517 | — | — | 1 | 4.90 |
| CHEMBL3265309 | — | — | 1 | 4.83 |
| CHEMBL3265301 | — | — | 1 | 4.79 |
| CHEMBL3265305 | — | — | 1 | 4.74 |
| CHEMBL3265312 | — | — | 1 | 4.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3265297 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL3265300 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3265298 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL3265299 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL3265313 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3265294 | — | IC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL3265295 | — | IC50 | = | 2310.0 | nM | 5.64 |
| CHEMBL1331211 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1564699 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3235895 | — | IC50 | = | 2760.0 | nM | 5.56 |
| CHEMBL3265310 | — | IC50 | = | 3870.0 | nM | 5.41 |
| CHEMBL3235886 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL1888104 | — | IC50 | = | 5010.0 | nM | 5.30 |
| CHEMBL3260033 | — | IC50 | = | 5030.0 | nM | 5.30 |
| CHEMBL3265292 | — | IC50 | = | 6180.0 | nM | 5.21 |
| CHEMBL2030270 | — | IC50 | = | 7120.0 | nM | 5.15 |
| CHEMBL1465938 | — | IC50 | = | 7170.0 | nM | 5.14 |
| CHEMBL3265293 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL3265290 | — | IC50 | = | 8730.0 | nM | 5.06 |
| CHEMBL1607263 | — | IC50 | = | 8680.0 | nM | 5.06 |
| CHEMBL3265303 | — | IC50 | = | 9590.0 | nM | 5.02 |
| CHEMBL3265291 | — | IC50 | = | 9680.0 | nM | 5.01 |
| CHEMBL3265296 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL3265311 | — | IC50 | = | 10950.0 | nM | 4.96 |
| CHEMBL1868007 | — | IC50 | = | 11570.0 | nM | 4.94 |
| CHEMBL1865517 | — | IC50 | = | 12580.0 | nM | 4.90 |
| CHEMBL3265309 | — | IC50 | = | 14880.0 | nM | 4.83 |
| CHEMBL3265301 | — | IC50 | = | 16200.0 | nM | 4.79 |
| CHEMBL3265305 | — | IC50 | = | 18270.0 | nM | 4.74 |
| CHEMBL3265312 | — | IC50 | = | 19680.0 | nM | 4.71 |
| CHEMBL3260041 | — | IC50 | = | 26840.0 | nM | 4.57 |
| CHEMBL3265304 | — | IC50 | = | 30200.0 | nM | 4.52 |
| CHEMBL3259874 | — | IC50 | = | 45080.0 | nM | 4.35 |
| CHEMBL3260039 | — | IC50 | = | 58430.0 | nM | 4.23 |
| CHEMBL3265306 | — | IC50 | = | 63770.0 | nM | 4.20 |
| CHEMBL3260034 | — | IC50 | = | 64900.0 | nM | 4.19 |
| CHEMBL3260040 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3260038 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3265302 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3260037 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3260036 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3260035 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3260032 | — | IC50 | - | — | - | |
| CHEMBL3265308 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3265307 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3265289 | — | IC50 | > | 100000.0 | nM | - |