Carboxyamidotriazole

Summary

Carboxyamidotriazole (CHEMBL95431) is a phase-3 clinical-stage small molecule; indicated across 9 conditions including non-small cell lung carcinoma and renal cell carcinoma.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 9 conditions
• Clinical trials: 7
• Chemistry: 424.7 Da · C17H12Cl3N5O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL95431
Name	Carboxyamidotriazole
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	108144
Molecular formula	C17H12Cl3N5O2
Molecular weight	424.7
InChIKey	WNRZHQBJSXRYJK-UHFFFAOYSA-N

SMILES: C1=CC(=CC=C1C(=O)C2=C(C=C(C=C2Cl)CN3C(=C(N=N3)C(=O)N)N)Cl)Cl

IUPAC name: 5-amino-1-[[3,5-dichloro-4-(4-chlorobenzoyl)phenyl]methyl]triazole-4-carboxamide

Also known as: Carboxyamidotriazole, L 651582, NSC-609974, SID4254373, SID50109733, SID485747, SID124753387, SID174006266, CARBOXYAMIDOTRIAZOLE, carboxyamidotriazole

Patent coverage: 3,112 distinct patent families (12,804 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Survival motor neuron protein, COUP transcription factor 2, Galanin receptor type 3, Cytochrome P450 2C9, Cytochrome P450 3A4, Hypoxia-inducible factor 1-alpha, Lethal factor.

Bioactivity

ChEMBL activities: 10 potent at pChembl ≥ 5 of 10 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
GALR3	6.52	IC50	303.1	nM	CHEMBL_ACT_12851418
CYP2C9	6.3	Potency	501.2	nM	CHEMBL_ACT_5037639
P15917	5.8	Potency	1585	nM	CHEMBL_ACT_4678919
HIF1A	5.5	Potency	3162	nM	CHEMBL_ACT_4128905
HIF1A	5.5	Potency	3162	nM	CHEMBL_ACT_4520727
CYP3A4	5.5	Potency	3162	nM	CHEMBL_ACT_5010301
CYP3A4	5.5	Potency	3162	nM	CHEMBL_ACT_5078715
CYP3A4	5.5	AC50	3162	nM	CHEMBL_ACT_6053653
SMN1	5.35	Potency	4467	nM	CHEMBL_ACT_3893835
NR2F2	5.04	IC50	9206	nM	CHEMBL_ACT_14335898

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

9 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
non-small cell lung carcinoma	3	MONDO:0005233	EFO:0003060
renal cell carcinoma	2	MONDO:0005086	EFO:0000681
gliosarcoma	2	MONDO:0016681	EFO:1001465
peritoneal neoplasm	2	MONDO:0006901	MONDO:0002087
fallopian tube neoplasm	2	MONDO:0021092	MONDO:0002158
kidney cancer	2	MONDO:0002367	MONDO:0002367
ovarian cancer	2	MONDO:0008170	MONDO:0008170
glioblastoma	2	MONDO:0018177	MONDO:0020690
neoplasm	1	MONDO:0005070	EFO:0000616

Clinical trials

Total trials: 7.

Phase distribution

Phase	Trials
PHASE2	4
PHASE1	2
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00003869	PHASE3	COMPLETED	Carboxyamidotriazole in Treating Patients With Stage III or Stage IV Non-small Cell Lung Cancer
NCT00004146	PHASE2	COMPLETED	Carboxyamidotriazole + RT in Treating Patients Newly Diagnosed Supratentorial GBM
NCT00005045	PHASE2	COMPLETED	Carboxyamidotriazole in Treating Patients With Advanced Kidney Cancer
NCT00006486	PHASE2	COMPLETED	Carboxyamidotriazole in Treating Patients With Metastatic Kidney Cancer
NCT00019461	PHASE2	COMPLETED	Carboxyamidotriazole in Treating Patients With Refractory or Recurrent Ovarian Epithelial, Fallopian Tube, or Primary Peritoneal Cancer
NCT00003249	PHASE1	COMPLETED	Carboxyamidotriazole and Ketoconazole in Treating Patients With Advanced Cancers
NCT00019019	PHASE1	COMPLETED	Carboxyamidotriazole and Paclitaxel in Treating Patients With Advanced Solid Tumors or Refractory Lymphomas

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

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).