Assay Detail
Binding
CHEMBL4256812
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Binding affinity to N-terminal His-tagged human recombinant XIAP BIR3 (253 to 347 residues) expressed in Escherichia coli BL21(DE3) Gold by isothermal titration calorimetric analysis
33
Total Activities
33
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 |
Publication
Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 33 | 6.46 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4288451 | — | — | 1 | 7.16 |
| CHEMBL4277802 | — | — | 1 | 7.09 |
| CHEMBL4278294 | — | — | 1 | 7.09 |
| CHEMBL4288478 | — | — | 1 | 7.07 |
| CHEMBL2063869 | GDC-0152 | 1.0 | 1 | 7.06 |
| CHEMBL4276715 | — | — | 1 | 6.96 |
| CHEMBL4282156 | — | — | 1 | 6.91 |
| CHEMBL4287773 | — | — | 1 | 6.88 |
| CHEMBL4283320 | — | — | 1 | 6.81 |
| CHEMBL4295015 | — | — | 1 | 6.81 |
| CHEMBL4288974 | — | — | 1 | 6.74 |
| CHEMBL4284370 | — | — | 1 | 6.72 |
| CHEMBL4278366 | — | — | 1 | 6.71 |
| CHEMBL4291176 | — | — | 1 | 6.69 |
| CHEMBL4292374 | — | — | 1 | 6.67 |
| CHEMBL4281757 | — | — | 1 | 6.64 |
| CHEMBL4286273 | — | — | 1 | 6.64 |
| CHEMBL4284639 | — | — | 1 | 6.57 |
| CHEMBL4294581 | — | — | 1 | 6.55 |
| CHEMBL4291873 | — | — | 1 | 6.49 |
| CHEMBL4291444 | — | — | 1 | 6.47 |
| CHEMBL4286676 | — | — | 1 | 6.46 |
| CHEMBL4279856 | — | — | 1 | 6.45 |
| CHEMBL4280168 | — | — | 1 | 6.41 |
| CHEMBL4285586 | — | — | 1 | 6.22 |
| CHEMBL4287457 | — | — | 1 | 6.14 |
| CHEMBL4288043 | — | — | 1 | 6.12 |
| CHEMBL4283597 | — | — | 1 | 6.11 |
| CHEMBL4290043 | — | — | 1 | 6.00 |
| CHEMBL4281250 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4288451 | — | Kd | = | 70.0 | nM | 7.16 |
| CHEMBL4277802 | — | Kd | = | 81.0 | nM | 7.09 |
| CHEMBL4278294 | — | Kd | = | 81.0 | nM | 7.09 |
| CHEMBL4288478 | — | Kd | = | 86.0 | nM | 7.07 |
| CHEMBL2063869 | GDC-0152 | Kd | = | 88.0 | nM | 7.06 |
| CHEMBL4276715 | — | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL4282156 | — | Kd | = | 122.0 | nM | 6.91 |
| CHEMBL4287773 | — | Kd | = | 133.0 | nM | 6.88 |
| CHEMBL4283320 | — | Kd | = | 155.0 | nM | 6.81 |
| CHEMBL4295015 | — | Kd | = | 155.0 | nM | 6.81 |
| CHEMBL4288974 | — | Kd | = | 182.0 | nM | 6.74 |
| CHEMBL4284370 | — | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL4278366 | — | Kd | = | 194.0 | nM | 6.71 |
| CHEMBL4291176 | — | Kd | = | 206.0 | nM | 6.69 |
| CHEMBL4292374 | — | Kd | = | 213.0 | nM | 6.67 |
| CHEMBL4286273 | — | Kd | = | 230.0 | nM | 6.64 |
| CHEMBL4281757 | — | Kd | = | 227.0 | nM | 6.64 |
| CHEMBL4284639 | — | Kd | = | 269.0 | nM | 6.57 |
| CHEMBL4294581 | — | Kd | = | 280.0 | nM | 6.55 |
| CHEMBL4291873 | — | Kd | = | 321.0 | nM | 6.49 |
| CHEMBL4291444 | — | Kd | = | 337.0 | nM | 6.47 |
| CHEMBL4286676 | — | Kd | = | 346.0 | nM | 6.46 |
| CHEMBL4279856 | — | Kd | = | 354.0 | nM | 6.45 |
| CHEMBL4280168 | — | Kd | = | 386.0 | nM | 6.41 |
| CHEMBL4285586 | — | Kd | = | 602.0 | nM | 6.22 |
| CHEMBL4287457 | — | Kd | = | 719.0 | nM | 6.14 |
| CHEMBL4288043 | — | Kd | = | 753.0 | nM | 6.12 |
| CHEMBL4283597 | — | Kd | = | 783.0 | nM | 6.11 |
| CHEMBL4290043 | — | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL4281250 | — | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL4276810 | — | Kd | = | 12000.0 | nM | 4.92 |
| CHEMBL4284657 | — | Kd | = | 13000.0 | nM | 4.89 |
| CHEMBL4280144 | — | Kd | = | 17000.0 | nM | 4.77 |