Bisantrene
drug drugOn this page
Also known as BisantrenoNSC-337766
Summary
Bisantrene (CHEMBL25336) is a phase-3 clinical-stage small molecule; indicated across 1 condition including acute myeloid leukemia.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Indications: 1 condition
- Clinical trials: 2
- Chemistry: 398.5 Da · C22H22N8
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL25336 |
| Name | Bisantrene |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 5351322 |
| Molecular formula | C22H22N8 |
| Molecular weight | 398.5 |
| InChIKey | NJSMWLQOCQIOPE-OCHFTUDZSA-N |
SMILES: C1NC(=NC1)N/N=C/C2=C3C(=C(C4=CC=CC=C24)/C=N/NC5=NCCN5)C=CC=C3
IUPAC name: N-[(E)-[10-[(E)-(4,5-dihydro-1H-imidazol-2-ylhydrazinylidene)methyl]anthracen-9-yl]methylideneamino]-4,5-dihydro-1H-imidazol-2-amine
Also known as: Bisantrene, Bisantreno, NSC-337766, BISANTRENE, bisantrene
Parent form; salt/anhydrous children: CHEMBL3989424
Patent coverage: 53 distinct patent families (85 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 78 (92%) 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
Broader ChEMBL bioactivity targets: 15 (assay-derived). Sample: Alpha-2A adrenergic receptor, D(1A) dopamine receptor, Muscarinic acetylcholine receptor M2, 5-hydroxytryptamine receptor 1A, Muscarinic acetylcholine receptor M1, Acetylcholinesterase, Sodium-dependent noradrenaline transporter, Sodium-dependent serotonin transporter, Alpha-1A adrenergic receptor, Mu-type opioid receptor, D(3) dopamine receptor, Sodium-dependent dopamine transporter, Adenosine receptor A3, RNA demethylase ALKBH5, NAD(P)H dehydrogenase [quinone] 1.
Bioactivity
ChEMBL activities: 13 potent at pChembl ≥ 5 of 15 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| ALKBH5 | 6.85 | IC50 | 140 | nM | CHEMBL_ACT_26037647 |
| ADRA1A | 5.83 | AC50 | 1470 | nM | CHEMBL_ACT_25218616 |
| HTR1A | 5.78 | AC50 | 1650 | nM | CHEMBL_ACT_25164751 |
| ADORA3 | 5.7 | AC50 | 2010 | nM | CHEMBL_ACT_25198498 |
| SLC6A4 | 5.65 | AC50 | 2250 | nM | CHEMBL_ACT_25151054 |
| CHRM2 | 5.56 | AC50 | 2740 | nM | CHEMBL_ACT_25195463 |
| ACHE | 5.41 | AC50 | 3880 | nM | CHEMBL_ACT_25142275 |
| DRD1 | 5.28 | AC50 | 5240 | nM | CHEMBL_ACT_25114937 |
| OPRM1 | 5.27 | AC50 | 5360 | nM | CHEMBL_ACT_25157902 |
| DRD3 | 5.22 | AC50 | 5960 | nM | CHEMBL_ACT_25194258 |
| CHRM1 | 5.2 | AC50 | 6370 | nM | CHEMBL_ACT_25209973 |
| SLC6A2 | 5.15 | AC50 | 7130 | nM | CHEMBL_ACT_25145727 |
| SLC6A3 | 5.02 | AC50 | 9570 | nM | CHEMBL_ACT_25124686 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
1 disease in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.
| Disease (in trials) | Phase | MONDO | EFO |
|---|---|---|---|
| acute myeloid leukemia | 2 | MONDO:0018874 | EFO:0000222 |
Clinical trials
Total trials: 2.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03820908 | PHASE2 | COMPLETED | Bisantrene for Relapsed /Refractory AML |
| NCT04989335 | PHASE2 | UNKNOWN | Bisantrene Combination for Resistant AML |
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).
Related Atlas pages
- In clinical trials for: acute myeloid leukemia