Tirilazad

Summary

Tirilazad (CHEMBL1630578) is a phase-3 clinical-stage small molecule (ATC N07XX01); indicated across 1 condition including spinal cord injury.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: N07XX01
• Indications: 1 condition
• Clinical trials: 1
• Chemistry: 624.9 Da · C38H52N6O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1630578
Name	Tirilazad
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	104903
ATC	N07XX01
Molecular formula	C38H52N6O2
Molecular weight	624.9
InChIKey	RBKASMJPSJDQKY-RBFSKHHSSA-N

SMILES: C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@@]4(C3=CC[C@@]2([C@H]1C(=O)CN5CCN(CC5)C6=NC(=NC(=C6)N7CCCC7)N8CCCC8)C)C

IUPAC name: (8S,10S,13S,14S,16R,17S)-17-[2-[4-(2,6-dipyrrolidin-1-ylpyrimidin-4-yl)piperazin-1-yl]acetyl]-10,13,16-trimethyl-6,7,8,12,14,15,16,17-octahydrocyclopenta[a]phenanthren-3-one

Also known as: Tirilazad, U 74006, U-74006, TIRILIZAD, TIRILAZAD, tirilazad

Parent form; salt/anhydrous children: CHEMBL3989513

Patent coverage: 341 distinct patent families (1,197 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: 21 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Tyrosine-protein kinase Fyn, Alpha-2A adrenergic receptor, Androgen receptor, Alpha-2C adrenergic receptor, Histamine H2 receptor, Epidermal growth factor receptor, D(1A) dopamine receptor, Progesterone receptor, Beta-2 adrenergic receptor.

Bioactivity

ChEMBL activities: 17 potent at pChembl ≥ 5 of 28 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HTR2C	6.42	Ki	376	nM	CHEMBL_ACT_7797940
CHRM2	6.37	AC50	431.5	nM	CHEMBL_ACT_25196248
HTR2A	6.24	Ki	572	nM	CHEMBL_ACT_7797936
HTR2C	6.14	IC50	718	nM	CHEMBL_ACT_7797939
FYN	5.95	IC50	1116	nM	CHEMBL_ACT_7797921
ADRA2C	5.94	Ki	1148	nM	CHEMBL_ACT_7827819
KCNH2	5.72	AC50	1900	nM	CHEMBL_ACT_25118651
HTR2A	5.7	IC50	2002	nM	CHEMBL_ACT_7797935
PTGS1	5.51	AC50	3054	nM	CHEMBL_ACT_25206666
PTGS1	5.42	AC50	3802	nM	CHEMBL_ACT_25205736
ADORA3	5.39	AC50	4068	nM	CHEMBL_ACT_25199125
PGR	5.2	AC50	6374	nM	CHEMBL_ACT_25204803
AR	5.18	AC50	6605	nM	CHEMBL_ACT_25203870
DRD1	5.15	AC50	7066	nM	CHEMBL_ACT_25115722
MAPK14	5.13	IC50	7406	nM	CHEMBL_ACT_7797915
ADRA2C	5.1	IC50	7898	nM	CHEMBL_ACT_7827818
DRD3	5.01	AC50	9694	nM	CHEMBL_ACT_25195019

Target pathways

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

Indications & clinical

Indications

1 indication (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
spinal cord injury	3	MONDO:0043797	MONDO:0043797

Clinical trials

Total trials: 1.

Phase distribution

Phase	Trials
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00004759	PHASE3	COMPLETED	Methylprednisolone Given by 24-Hour or 48-Hour Infusion Versus Tirilazad for Acute Spinal Cord Injury

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).