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Target Report Card

Target Name and Classification

Target ID CHEMBL5145
Target Type SINGLE PROTEIN
Preferred Name Serine/threonine-protein kinase B-raf
Synonyms BRAF | BRAF1 | Proto-oncogene B-Raf | RAFB1 | Serine/threonine-protein kinase B-raf | p94 | v-Raf murine sarcoma viral oncogene homolog B1
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > tkl protein kinase group > tkl protein kinase raf family

Target Components

Component Description Relationship Accession
Serine/threonine-protein kinase B-raf SINGLE PROTEIN P15056

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL3559685 RAF serine/threonine protein kinase PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1200485 SORAFENIB TOSYLATE Serine/threonine-protein kinase B-raf inhibitor 4 FDA
CHEMBL1229517 VEMURAFENIB Serine/threonine-protein kinase B-raf inhibitor 4 FDA
CHEMBL1946170 REGORAFENIB Serine/threonine-protein kinase B-raf inhibitor 4 Expert
CHEMBL2105729 DABRAFENIB MESYLATE Serine/threonine-protein kinase B-raf inhibitor 4 DailyMed
CHEMBL3301612 ENCORAFENIB Serine/threonine-protein kinase B-raf inhibitor 3 DOI PubMed
CHEMBL558752 CHIR-265 Serine/threonine-protein kinase B-raf inhibitor 2 PubMed PubMed
CHEMBL3545027 XL-281 Serine/threonine-protein kinase B-raf inhibitor 2 Other Other PubMed PubMed
CHEMBL2029988 CEP-32496 Serine/threonine-protein kinase B-raf inhibitor 1 Other
CHEMBL3545005 PLX-8394 Serine/threonine-protein kinase B-raf inhibitor 1 Other PubMed PubMed
CHEMBL3545080 RG-7256 Serine/threonine-protein kinase B-raf inhibitor 1 PubMed
CHEMBL3545195 LY-3009120 Serine/threonine-protein kinase B-raf inhibitor 1 PubMed
CHEMBL3545246 BGB-283 Serine/threonine-protein kinase B-raf inhibitor 1 PubMed
CHEMBL3545263 LGX-806 Serine/threonine-protein kinase B-raf inhibitor 1
CHEMBL3545296 ARQ-736 Serine/threonine-protein kinase B-raf inhibitor 1 DOI Other PubMed
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000157764
Ensembl ENSG00000157764
GO Cellular Component GO:0005634 (nucleus)
GO:0005737 (cytoplasm)
GO:0005739 (mitochondrion)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0016020 (membrane)
GO:0043005 (neuron projection)
GO:0043231 (intracellular membrane-bounded organelle)
GO:0044297 (cell body)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0004672 (protein kinase activity)
GO:0004674 (protein serine/threonine kinase activity)
GO:0004709 (MAP kinase kinase kinase activity)
GO:0005057 (receptor signaling protein activity)
GO:0005509 (calcium ion binding)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0031267 (small GTPase binding)
GO:0031434 (mitogen-activated protein kinase kinase binding)
GO:0042802 (identical protein binding)
GO:0046872 (metal ion binding)
GO:0046982 (protein heterodimerization activity)
GO Biological Process GO:0000165 (MAPK cascade)
GO:0000186 (activation of MAPKK activity)
GO:0002318 (myeloid progenitor cell differentiation)
GO:0006468 (protein phosphorylation)
GO:0007165 (signal transduction)
GO:0008542 (visual learning)
GO:0009887 (organ morphogenesis)
GO:0010628 (positive regulation of gene expression)
GO:0010764 (negative regulation of fibroblast migration)
GO:0015758 (glucose transport)
GO:0016310 (phosphorylation)
GO:0030154 (cell differentiation)
GO:0030878 (thyroid gland development)
GO:0033138 (positive regulation of peptidyl-serine phosphorylation)
GO:0035019 (somatic stem cell population maintenance)
GO:0035556 (intracellular signal transduction)
GO:0035690 (cellular response to drug)
GO:0042127 (regulation of cell proliferation)
GO:0043066 (negative regulation of apoptotic process)
GO:0043367 (CD4-positive, alpha-beta T cell differentiation)
GO:0043368 (positive T cell selection)
GO:0043434 (response to peptide hormone)
GO:0043524 (negative regulation of neuron apoptotic process)
GO:0046632 (alpha-beta T cell differentiation)
GO:0048538 (thymus development)
GO:0048679 (regulation of axon regeneration)
GO:0048680 (positive regulation of axon regeneration)
GO:0050772 (positive regulation of axonogenesis)
GO:0051291 (protein heterooligomerization)
GO:0051496 (positive regulation of stress fiber assembly)
GO:0051591 (response to cAMP)
GO:0060291 (long-term synaptic potentiation)
GO:0060323 (head morphogenesis)
GO:0060324 (face development)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
GO:0071277 (cellular response to calcium ion)
GO:0090150 (establishment of protein localization to membrane)
GO:1900026 (positive regulation of substrate adhesion-dependent cell spreading)
GO:2000301 (negative regulation of synaptic vesicle exocytosis)
GO:2000352 (negative regulation of endothelial cell apoptotic process)
Wikipedia BRAF_(gene)

Target Cross References - Protein

canSAR P15056
CGD Noonan syndrome; Cardiofaciocutaneous syndrome; LEOPARD syndrome
Human Protein Atlas ENSG00000157764
IntAct P15056
Guide to Pharmacology 1943
Open Targets ENSG00000157764
PharmGKB PA25408
Pharos P15056 (Tclin)
Reactome R-HSA-1295596 (Spry regulation of FGF signaling.)
R-HSA-170968 (Frs2-mediated activation.)
R-HSA-170984 (ARMS-mediated activation.)
R-HSA-187706 (Signalling to p38 via RIT and RIN.)
R-HSA-442742 (CREB phosphorylation through the activation of Ras.)
R-HSA-5673000 (RAF activation.)
R-HSA-5674135 (MAP2K and MAPK activation.)
R-HSA-5674499 (Negative feedback regulation of MAPK pathway.)
R-HSA-5675221 (Negative regulation of MAPK pathway.)
UniProt A4D1T4 B6HY61 B6HY62 B6HY63 B6HY64 B6HY65 B6HY66 P15056 Q13878 Q3MIN6 Q9UDP8 Q9Y6T3

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR001245 (Ser-Thr/Tyr_kinase_cat_dom.)
IPR002219 (PE/DAG-bd.)
IPR003116 (RBD_dom.)
IPR008271 (Ser/Thr_kinase_AS.)
IPR011009 (Kinase-like_dom.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR020454 (DAG/PE-bd.)
IPR029071 (Ubiquitin-rel_dom.)
Pfam PF00130 (C1_1)
PF02196 (RBD)
PF07714 (Pkinase_Tyr)

Target Cross References - Structure

PDBe 1UWH 1UWJ 2FB8 3C4C 3D4Q 3IDP 3II5 3NY5 3OG7 3PPJ 3PPK 3PRF 3PRI 3PSB 3PSD 3Q4C 3Q96 3SKC 3TV4 3TV6 4DBN 4E26 4E4X 4EHE More...
CREDO 1UWH 1UWJ 2FB8 3C4C 3D4Q 3IDP 3II5 3NY5 3OG7 3PPJ 3PPK 3PRF 3PRI 3PSB 3PSD 3Q4C 3Q96 3SKC 3TV4 3TV6 4DBN 4E26 4E4X 4EHE More...
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