Compound Detail
CHEMBL1554
DACTINOMYCIN 💊 Approved Drug
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💊 Approved Drug
Cc1c2oc3c(C)ccc(C(=O)N[C@@H]4C(=O)N[C@H](C(C)C)C(=O)N5CCC[C@H]5C(=O)N(C)CC(=O)N(C)[C@@H](C(C)C)C(=O)O[C@@H]4C)c3nc-2c(C(=O)N[C@@H]2C(=O)N[C@H](C(C)C)C(=O)N3CCC[C@H]3C(=O)N(C)CC(=O)N(C)[C@@H](C(C)C)C(=O)O[C@@H]2C)c(N)c1=O
Basic Information
| ChEMBL ID | CHEMBL1554 |
| Name | DACTINOMYCIN |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | RJURFGZVJUQBHK-IIXSONLDSA-N |
| Therapeutic | ✓ Yes |
49
Targets
148
Activities
3
Assay Types
1
PK Parameters
20
Publications
19
Known Names
20
Indications
1
Mechanisms
Molecular Properties
1255.4
MW (Da)
Drug Information
| Molecule Type | Protein |
| First Approval | 1964 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| DNA inhibitor | INHIBITOR | DNA | ✓ | ✓ |
Indications
Neoplasms Wilms Tumor Brain Neoplasms Choriocarcinoma Choriocarcinoma Choroid Plexus Neoplasms Gestational Trophoblastic Disease Hydatidiform Mole Kidney Neoplasms Leukemia Lymphoma Rhabdomyosarcoma Rhabdomyosarcoma, Alveolar Rhabdomyosarcoma, Embryonal Sarcoma Sarcoma Sarcoma, Ewing Central Nervous System Neoplasms Melanoma Testicular Neoplasms
ATC Classification
L01DA01
dactinomycin
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ANTINEOPLASTIC AGENTS
Activity Summary
IC50 140 meas. best 10.1
EC50 7 meas. best 9.7
Kd 1 meas. best 4.05
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| C8166 CHEMBL614533 | IC50 | 10.1 | 9.4333 | 0.1 | 3 |
| A549 CHEMBL392 | EC50 | 9.7 | 9.7 | 0.2 | 1 |
| P388 CHEMBL389 | IC50 | 9.7 | 7.6533 | 0.2 | 3 |
| PC-3 CHEMBL390 | EC50 | 9.56 | 9.56 | 0.3 | 1 |
| HeLa CHEMBL399 | IC50 | 9.4 | 8.0873 | 0.4 | 15 |
| A2780 CHEMBL614004 | IC50 | 9.1 | 9.1 | 0.8 | 2 |
| MT4 CHEMBL388 | IC50 | 9.05 | 9.02 | 0.9 | 5 |
| KB CHEMBL398 | IC50 | 9.0 | 7.62 | 1.0 | 5 |
| CCRF-SB CHEMBL614542 | IC50 | 9.0 | 8.775 | 1.0 | 4 |
| Vero CHEMBL391 | IC50 | 9.0 | 7.0522 | 1.0 | 9 |
| Unchecked CHEMBL612545 | IC50 | 9.0 | 8.44 | 1.0 | 6 |
| MOLT-4 CHEMBL614177 | IC50 | 9.0 | 9.0 | 1.0 | 3 |
| CCRF-CEM CHEMBL382 | IC50 | 9.0 | 8.3533 | 1.0 | 6 |
| G-361 CHEMBL614036 | IC50 | 9.0 | 8.805 | 1.0 | 4 |
| SK-MEL-28 CHEMBL614919 | IC50 | 8.7 | 8.7 | 2.0 | 2 |
| Raji CHEMBL614628 | IC50 | 8.7 | 8.7 | 2.0 | 2 |
| HT-29 CHEMBL384 | IC50 | 8.54 | 7.64 | 2.9 | 8 |
| NON-PROTEIN TARGET CHEMBL3879801 | IC50 | 8.52 | 7.8333 | 3.0 | 3 |
| 5637 CHEMBL612565 | IC50 | 8.52 | 8.52 | 3.0 | 3 |
| WIL2-NS CHEMBL612810 | IC50 | 8.52 | 8.52 | 3.0 | 2 |
| U2OS CHEMBL615023 | IC50 | 8.49 | 8.49 | 3.2 | 1 |
| HEp-2 CHEMBL614735 | IC50 | 8.4 | 8.028 | 4.0 | 5 |
| SK-MES-1 CHEMBL614923 | IC50 | 8.4 | 8.4 | 4.0 | 1 |
| Jurkat CHEMBL397 | IC50 | 8.35 | 8.35 | 4.5 | 1 |
| Homo sapiens CHEMBL372 | IC50 | 8.35 | 8.35 | 4.5 | 1 |
| ACHN CHEMBL614519 | IC50 | 8.3 | 8.3 | 5.0 | 4 |
| ADMET CHEMBL612558 | IC50 | 8.3 | 7.25 | 5.0 | 4 |
| MCF7 CHEMBL387 | IC50 | 8.22 | 7.6138 | 6.0 | 8 |
| CRL-7065 cell line CHEMBL614151 | IC50 | 8.15 | 8.15 | 7.0 | 1 |
| A549 CHEMBL392 | IC50 | 8.14 | 7.45 | 7.2 | 4 |
| NCI-H460 CHEMBL396 | IC50 | 8.1 | 8.1 | 8.0 | 1 |
| DU-145 CHEMBL613508 | IC50 | 8.1 | 8.1 | 8.0 | 1 |
| HepG2 CHEMBL395 | IC50 | 8.0 | 8.0 | 10.0 | 3 |
| SF-268 CHEMBL613977 | IC50 | 7.8 | 7.8 | 16.0 | 1 |
| L1210 CHEMBL386 | IC50 | 7.72 | 7.07 | 19.0 | 2 |
| HL-60 CHEMBL383 | IC50 | 7.7 | 7.7 | 20.0 | 1 |
| RKO CHEMBL614879 | IC50 | 7.52 | 7.52 | 30.0 | 1 |
| Plasmodium falciparum CHEMBL364 | EC50 | 6.67 | 6.4125 | 214.5 | 4 |
| L02 CHEMBL4296457 | IC50 | 6.3 | 6.3 | 500.0 | 1 |
| SK-OV-3 CHEMBL614925 | IC50 | 6.21 | 6.21 | 620.0 | 1 |
| SK-BR-3 CHEMBL613834 | IC50 | 6.17 | 6.17 | 680.0 | 1 |
| BEAS-2B CHEMBL4296403 | IC50 | 6.16 | 6.16 | 700.0 | 1 |
| PC-3 CHEMBL390 | IC50 | 6.15 | 6.15 | 710.0 | 1 |
| NHDF CHEMBL614200 | IC50 | 5.79 | 5.79 | 1630.0 | 1 |
| Nucleic Acid CHEMBL345 | EC50 | 5.37 | 5.37 | 4300.0 | 1 |
| Growth factor receptor-bound protein 2 CHEMBL4830 | IC50 | 5.3 | 5.3 | 5000.0 | 1 |
| Growth factor receptor-bound protein 2 CHEMBL3663 | IC50 | 5.3 | 5.3 | 5000.0 | 1 |
| Discoidin domain-containing receptor 2 CHEMBL5122 | IC50 | 5.05 | 5.05 | 9000.0 | 1 |
| B16-F10 CHEMBL612656 | IC50 | 4.87 | 4.87 | 13400.0 | 1 |
| Calf thymus DNA CHEMBL612514 | IC50 | 4.46 | 4.46 | 35000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| Ka | 1.56 | 10'6/M | Bos taurus |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.6019/CHEMBL3885881 | Rattus norvegicus | 408 |
| 21051535 | 10.1124/dmd.110.034629 | ADMET | 21 |
| 226705 | 10.1021/jm00195a008 | Bacterial DNA-directed RNA polymerase | 19 |
| 16472241 | 10.2174/1570163043334794 | Hepatotoxicity | 18 |
| 7143358 | 10.1021/jm00352a023 | P388 | 17 |
| 3351854 | 10.1021/jm00399a014 | MC-38 | 15 |
| 22194678 | 10.1371/journal.pcbi.1002310 | Hepatotoxicity | 14 |
| 226705 | 10.1021/jm00195a008 | P388 | 12 |
| 15646539 | 10.1016/s0399-8320(04)95062-2 | Unchecked | 11 |
| 3397991 | 10.1021/jm00403a010 | Mus musculus | 10 |
| 448678 | 10.1021/jm00193a009 | P388 | 9 |
| 226705 | 10.1021/jm00195a008 | L1210 | 8 |
| 34270246 | 10.1021/acs.jnatprod.1c00294 | Staphylococcus aureus | 8 |
| 11602674 | - | ATP-dependent translocase ABCB1 | 8 |
| 15646539 | 10.1016/s0399-8320(04)95062-2 | NON-PROTEIN TARGET | 8 |
| 3351854 | 10.1021/jm00399a014 | Rattus norvegicus | 7 |
| 97381 | 10.1021/jm00205a004 | Calf thymus DNA | 7 |
| 16420056 | 10.1021/jm050772b | MOLT-3 | 7 |
| 16933866 | 10.1021/np060063g | NON-PROTEIN TARGET | 6 |
| 20194695 | 10.1128/aac.01730-09 | Human betaherpesvirus 5 | 6 |
Data from ChEMBL 36 via Core Engine