Compound Detail

CHEMBL3977543

BELVARAFENIB

🧪 Phase II

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🧪 Phase II

Cc1ccc2c(Nc3cccc(Cl)c3F)nccc2c1NC(=O)c1csc2c(N)ncnc12

ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID	CHEMBL3977543
Name	BELVARAFENIB
Phase	Phase II
Structure Type	MOL
InChI Key	KVCQTKNUUQOELD-UHFFFAOYSA-N

Known Names

Belvarafenib

Targets

Activities

Assay Types

PK Parameters

Publications

Known Names

Indications

Mechanisms

Molecular Properties

478.9

MW (Da)

5.92

ALogP

HBA

HBD

105.8

PSA (Å²)

0.30

QED

Ro5 Violations

Rot. Bonds

Drug Information

Molecule Type	Small molecule
Chirality	Achiral

USAN Stem

-rafenib

Extended Properties

Molecular Formula	C23H16ClFN6OS
MW	478.94
Aromatic Rings	5
Heavy Atoms	33
NP-Likeness	-1.52

Mechanism of Action

Mechanism	Action Type	Target	Direct	Efficacy
RAF serine/threonine protein kinase inhibitor	INHIBITOR	RAF serine/threonine protein kinase	✓	✓

Indications

Neoplasms Neoplasms Melanoma

Activity Summary

IC50 11 meas. best 8.3

Target Activity Profile

Target	Type	Best pChEMBL	Mean pChEMBL	Best (nM)	# Data
RAF proto-oncogene serine/threonine-protein kinase CHEMBL1906	IC50	8.3	7.97	5.0	2
Serine/threonine-protein kinase B-raf CHEMBL5145	IC50	8.15	7.5975	7.0	4
Macrophage colony-stimulating factor 1 receptor CHEMBL1844	IC50	8.0	8.0	10.0	2
Epithelial discoidin domain-containing receptor 1 CHEMBL5319	IC50	7.64	7.64	23.0	1
Discoidin domain-containing receptor 2 CHEMBL5122	IC50	7.36	7.36	44.0	1
Serine/threonine-protein kinase A-Raf CHEMBL1169596	IC50	6.82	6.82	152.0	1

Activity Data Samples

Top measurements by pChEMBL value

Target	Type	Rel.	Value	Units	pChEMBL	Assay	PubMed
RAF proto-oncogene serine/threonine-protein kinase	IC50	=	5.0	nM	8.3	Kinase Activity: The compounds prepared in Examples were tested for inhibitory a...	-
Serine/threonine-protein kinase B-raf	IC50	=	7.0	nM	8.15	Kinase Activity: The compounds prepared in Examples were tested for inhibitory a...	-
Serine/threonine-protein kinase B-raf	IC50	=	9.0	nM	8.05	Inhibition of B-RAF V600E mutant (unknown origin)	38954961
Macrophage colony-stimulating factor 1 receptor	IC50	=	10.0	nM	8.0	Kinase Activity: The compounds prepared in Examples were tested for inhibitory a...	-
Macrophage colony-stimulating factor 1 receptor	IC50	=	10.0	nM	8.0	Kinase Activity: The compounds prepared in Examples were tested for inhibitory a...	-
Epithelial discoidin domain-containing receptor 1	IC50	=	23.0	nM	7.64	Kinase Activity: The compounds prepared in Examples were tested for inhibitory a...	-
RAF proto-oncogene serine/threonine-protein kinase	IC50	=	23.0	nM	7.64	Inhibition of C-RAF (unknown origin)	38954961
Discoidin domain-containing receptor 2	IC50	=	44.0	nM	7.36	Kinase Activity: The compounds prepared in Examples were tested for inhibitory a...	-
Serine/threonine-protein kinase B-raf	IC50	=	56.0	nM	7.25	Kinase Activity: The compounds prepared in Examples were tested for inhibitory a...	-
Serine/threonine-protein kinase B-raf	IC50	=	116.0	nM	6.94	Inhibition of B-RAF (unknown origin)	38954961
Serine/threonine-protein kinase A-Raf	IC50	=	152.0	nM	6.82	Inhibition of ARAF (unknown origin)	38954961

Literature References

PubMed	DOI	Target Context	# Activities
38954961	10.1016/j.ejmech.2024.116631	Serine/threonine-protein kinase B-raf	2
38954961	10.1016/j.ejmech.2024.116631	Serine/threonine-protein kinase A-Raf	1
38954961	10.1016/j.ejmech.2024.116631	RAF proto-oncogene serine/threonine-protein kinase	1

Data from ChEMBL 36 via Core Engine