Assay Detail
Binding
CHEMBL3858905
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Inhibition of full length recombinant human His-tagged BTK expressed in baculovirus using fluoresceinated peptide incubated for 60 mins by fluorescent assay
22
Total Activities
16
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
Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 8.54 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3899411 | — | — | 1 | 9.57 |
| CHEMBL3896019 | — | — | 1 | 9.35 |
| CHEMBL3900554 | BMS-986142 | 2.0 | 2 | 9.30 |
| CHEMBL3931086 | — | — | 1 | 9.19 |
| CHEMBL3936249 | — | — | 3 | 9.00 |
| CHEMBL3936156 | — | — | 2 | 8.92 |
| CHEMBL3897349 | — | — | 1 | 8.82 |
| CHEMBL3952795 | — | — | 1 | 8.66 |
| CHEMBL3908310 | — | — | 3 | 8.64 |
| CHEMBL3918580 | — | — | 1 | 8.59 |
| CHEMBL3944049 | — | — | 1 | 8.59 |
| CHEMBL3941224 | — | — | 1 | 8.59 |
| CHEMBL3976719 | — | — | 1 | 8.57 |
| CHEMBL3977725 | — | — | 1 | 8.29 |
| CHEMBL3891391 | — | — | 1 | 7.96 |
| CHEMBL3939772 | — | — | 1 | 7.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3899411 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL3896019 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL3900554 | BMS-986142 | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3931086 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL3936249 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3936156 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3897349 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3936156 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3952795 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3908310 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3918580 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3944049 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3941224 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3976719 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3908310 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3936249 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3908310 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3977725 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3891391 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3900554 | BMS-986142 | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3939772 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3936249 | — | IC50 | = | 130.0 | nM | 6.89 |