Terevalefim

Summary

Terevalefim (CHEMBL4650326) is a phase-3 clinical-stage small molecule targeting MET; indicated across 3 conditions including acute kidney injury.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (MET)
• Indications: 3 conditions
• Clinical trials: 7
• Chemistry: 176.24 Da · C9H8N2S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4650326
Name	Terevalefim
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	5714038
Molecular formula	C9H8N2S
Molecular weight	176.24
InChIKey	FOHWAQGURRYJFK-ONEGZZNKSA-N

SMILES: C1=CSC(=C1)/C=C/C2=CC=NN2

IUPAC name: 5-[(E)-2-thiophen-2-ylethenyl]-1H-pyrazole

Also known as: Ang-3777, ANG-3777, BB-3, BB3, Refanalin, SNV-003, Terevalefim, TEREVALEFIM

Patent coverage: 59 distinct patent families (176 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 144 (82%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
MET	MET proto-oncogene, receptor tyrosine kinase	Activation		2.4%	P08581

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): MET.

Top Reactome pathways

44 total, by targets touching each:

Pathway	Targets	Genes
PIP3 activates AKT signaling	1	MET
Developmental Biology	1	MET
Signal Transduction	1	MET
Disease	1	MET
Negative regulation of the PI3K/AKT network	1	MET
Generic Transcription Pathway	1	MET
PI3K/AKT Signaling in Cancer	1	MET
Constitutive Signaling by Aberrant PI3K in Cancer	1	MET
Semaphorin interactions	1	MET
Sema4D in semaphorin signaling	1	MET
Sema4D mediated inhibition of cell attachment and migration	1	MET
Axon guidance	1	MET
Diseases of signal transduction by growth factor receptors and second messengers	1	MET
Infectious disease	1	MET
RAF/MAP kinase cascade	1	MET
MAPK family signaling cascades	1	MET
MAPK1/MAPK3 signaling	1	MET
Signaling by MET	1	MET
MET Receptor Activation	1	MET
Negative regulation of MET activity	1	MET
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	1	MET
RNA Polymerase II Transcription	1	MET
Gene expression (Transcription)	1	MET
MET activates RAS signaling	1	MET
MET activates PI3K/AKT signaling	1	MET
MET activates PTPN11	1	MET
MET activates PTK2 signaling	1	MET
InlB-mediated entry of Listeria monocytogenes into host cell	1	MET
MET interacts with TNS proteins	1	MET
MET activates RAP1 and RAC1	1	MET

Dominant GO biological processes

GO term	Targets
endothelial cell morphogenesis	1
liver development	1
cell surface receptor signaling pathway	1
cell surface receptor protein tyrosine kinase signaling pathway	1
negative regulation of autophagy	1
neuron differentiation	1
pancreas development	1
positive regulation of transcription by RNA polymerase II	1
hepatocyte growth factor receptor signaling pathway	1
branching morphogenesis of an epithelial tube	1
positive chemotaxis	1
excitatory postsynaptic potential	1
semaphorin-plexin signaling pathway	1
negative regulation of hydrogen peroxide-mediated programmed cell death	1
positive regulation of endothelial cell chemotaxis	1

Indications & clinical

Indications

3 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
acute kidney injury	2	MONDO:0002492	HP:0001919

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 7.

Phase distribution

Phase	Trials
PHASE2	5
PHASE3	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02474667	PHASE3	UNKNOWN	Reduce the Severity of DGF in Recipients of a Deceased Donor Kidney
NCT01286727	PHASE2	UNKNOWN	Study to Improve Renal Function After Kidney Transplantation
NCT01539590	PHASE2	TERMINATED	Study to Evaluate the Safety and Activity of BB3 to Treat Heart Attack
NCT01561599	PHASE2	UNKNOWN	Study on Delayed Graft Function Using Paired Kidneys
NCT02771509	PHASE2	UNKNOWN	Study to Prevent Acute Kidney Injury After Cardiac Surgery Involving Cardiopulmonary Bypass
NCT04459676	PHASE2	UNKNOWN	Study to Assess Efficacy and Safety Relative to Standard of Care in Patients With COVID-19 Pneumonia
NCT04958187	PHASE1	UNKNOWN	Study to Evaluate the Pharmacokinetics of ANG-3777 in Hemodialysis Subjects

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

84 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
AFATINIB	ChEMBL + PubChem	Phase 4 (approved)	MET
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	MET
PAZOPANIB	ChEMBL + PubChem	Phase 4 (approved)	MET
AFATINIB DIMALEATE	ChEMBL	Phase 4 (approved)	MET
AXITINIB	ChEMBL	Phase 4 (approved)	MET
BOSUTINIB	ChEMBL	Phase 4 (approved)	MET
BRIGATINIB	ChEMBL	Phase 4 (approved)	MET
CABOZANTINIB	ChEMBL	Phase 4 (approved)	MET
CABOZANTINIB S-MALATE	ChEMBL	Phase 4 (approved)	MET
CAPMATINIB	ChEMBL	Phase 4 (approved)	MET
CERITINIB	ChEMBL	Phase 4 (approved)	MET
DABRAFENIB	ChEMBL	Phase 4 (approved)	MET
ENSARTINIB	ChEMBL	Phase 4 (approved)	MET
ENTRECTINIB	ChEMBL	Phase 4 (approved)	MET
ERLOTINIB	ChEMBL	Phase 4 (approved)	MET
FEDRATINIB	ChEMBL	Phase 4 (approved)	MET
GEFITINIB	ChEMBL	Phase 4 (approved)	MET
INFIGRATINIB	ChEMBL	Phase 4 (approved)	MET
MIDOSTAURIN	ChEMBL	Phase 4 (approved)	MET
NERATINIB	ChEMBL	Phase 4 (approved)	MET
NINTEDANIB	ChEMBL	Phase 4 (approved)	MET
PALBOCICLIB	ChEMBL	Phase 4 (approved)	MET
SORAFENIB	ChEMBL	Phase 4 (approved)	MET
SUNITINIB	ChEMBL	Phase 4 (approved)	MET
TEPOTINIB	ChEMBL	Phase 4 (approved)	MET
TIVOZANIB	ChEMBL	Phase 4 (approved)	MET
VANDETANIB	ChEMBL	Phase 4 (approved)	MET
CANERTINIB	ChEMBL	Phase 3	MET
CEDIRANIB	ChEMBL	Phase 3	MET
DACTOLISIB	ChEMBL	Phase 3	MET
ENZASTAURIN	ChEMBL	Phase 3	MET
EPIGALOCATECHIN GALLATE	ChEMBL	Phase 3	MET
LESTAURTINIB	ChEMBL	Phase 3	MET
LINIFANIB	ChEMBL	Phase 3	MET
LINSITINIB	ChEMBL	Phase 3	MET
POZIOTINIB	ChEMBL	Phase 3	MET
QUERCETIN	ChEMBL	Phase 3	MET
RIGOSERTIB	ChEMBL	Phase 3	MET
SAVOLITINIB	ChEMBL	Phase 3	MET
SITRAVATINIB	ChEMBL	Phase 3	MET
TIVANTINIB	ChEMBL	Phase 3	MET
ALTIRATINIB	ChEMBL	Phase 2	MET
AMG-208	ChEMBL	Phase 2	MET
AMG-337	ChEMBL	Phase 2	MET
AT-9283	ChEMBL	Phase 2	MET
BEMCENTINIB	ChEMBL	Phase 2	MET
BI-2536	ChEMBL	Phase 2	MET
BMS-754807	ChEMBL	Phase 2	MET
BMS-777607	ChEMBL	Phase 2	MET
CENISERTIB	ChEMBL	Phase 2	MET
CEP-32496	ChEMBL	Phase 2	MET
DALMELITINIB	ChEMBL	Phase 2	MET
DECERNOTINIB	ChEMBL	Phase 2	MET
DEFOSBARASERTIB	ChEMBL	Phase 2	MET
ELLAGIC ACID	ChEMBL	Phase 2	MET
ELZOVANTINIB	ChEMBL	Phase 2	MET
ENVONALKIB	ChEMBL	Phase 2	MET
FORETINIB	ChEMBL	Phase 2	MET
GLESATINIB	ChEMBL	Phase 2	MET
GOLVATINIB	ChEMBL	Phase 2	MET