Activity-based BRAF mutant kinase panel for compound profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
BRAF
Enzyme
Human BRAF
HGNC
BRAF
Synonym
B-Raf proto-oncogene serine/threonine-protein kinase, B-Raf proto-oncogene serine/threonine-protein, kinase, BRAF1, RAFB1
Assay Properties
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s (nM)
| Mutant | Staurosporine | Ro 31-8220 | GW5074 | H-89 | Rottlerin |
|---|---|---|---|---|---|
| WT | n.a. | n.a. | 24 | n.a. | n.a. |
| d485-489/P490Y | >100,000 | 17,700 | 42 | >100,000 | >100,000 |
| G464V | >100,000 | 14,600 | 87 | >100,000 | >100,000 |
| G469A | >100,000 | 19,500 | 8.0 | >100,000 | >100,000 |
| R506_K507insVLR | >100,000 | 15,100 | 20 | >100,000 | >100,000 |
| L597V | >100,000 | 9,700 | 2.8 | >100,000 | >100,000 |
| T599_V600insT | >100,000 | 8,000 | 6.0 | >100,000 | >100,000 |
| V599E | n.a. | n.a. | 8.5 | n.a. | n.a. |
| V600A | >100,000 | 8,700 | 3.2 | >100,000 | >100,000 |
| V600D | >100,000 | 8,800 | 1.7 | >100,000 | >100,000 |
| V600K | >100,000 | 7,800 | 2.2 | >100,000 | >100,000 |
| K601E | >100,000 | 5,800 | 5.0 | >100,000 | >100,000 |
| FAM131B | >100,000 | 12,000 | 3.7 | >100,000 | >100,000 |
| KIAA1549 (Kex15Bex9) | >100,000 | 14,700 | 2.3 | >100,000 | >100,000 |
| KIAA1549 (Kex16Bex9) | 13,000 | 11,300 | 13 | >100,000 | >100,000 |
| SRGAP3 | >100,000 | 12,500 | 2.7 | >100,000 | >100,000 |
Screening Location
Malvern, USA
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