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Compound Detail

CHEMBL43452

POMALIDOMIDE
💊 Approved Drug
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💊 Approved Drug
Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL43452
Name POMALIDOMIDE
Phase Approved
Structure Type MOL
InChI Key UVSMNLNDYGZFPF-UHFFFAOYSA-N
Therapeutic ✓ Yes

Known Names

Actimid CC-4047 IMID 3 IMID-3 IMID3 Imnovid Imnovid (previously pomalidomide celgene) Pomalidomida Pomalidomide Pomalidomide accord Pomalidomide krka Pomalidomide viatris +2 more
20
Targets
40
Activities
4
Assay Types
6
PK Parameters
20
Publications
14
Known Names
20
Indications
1
Mechanisms

Molecular Properties

273.2
MW (Da)
-0.33
ALogP
5
HBA
2
HBD
109.6
PSA (Ų)
0.54
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2013
Availability Prescription
Chirality Racemic

Routes of Administration

Oral

Flags

Black Box Warning Natural Product
USAN Stem -domide
USAN Year 2006

Extended Properties

Molecular Formula C13H11N3O4
MW 273.25
Aromatic Rings 1
Heavy Atoms 20
NP-Likeness -0.21

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
CRL4(CRBN) E3 ubiquitin ligase inhibitor INHIBITOR CRL4(CRBN) E3 ubiquitin ligase ✓ ✓

Indications

Immune System Diseases Multiple Myeloma Primary Myelofibrosis Primary Myelofibrosis Amyloidosis Amyloidosis, Familial Central Nervous System Neoplasms Graft vs Host Disease Leukemia, Plasma Cell Lung Diseases, Interstitial Lymphoma, Large B-Cell, Diffuse Medulloblastoma Myeloproliferative Disorders Neoplasms, Plasma Cell Plasmacytoma Polycythemia Vera Prostatic Neoplasms, Castration-Resistant Pulmonary Fibrosis Sarcoma Sarcoma, Kaposi

ATC Classification

L04AX06
pomalidomide
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: IMMUNOSUPPRESSANTS

Drug Warnings

Black Box Warning
vascular toxicity
Country: United States
Black Box Warning
teratogenicity
Country: United States

Activity Summary

IC50 29 meas. best 7.89
EC50 6 meas. best 8.1
Ki 3 meas. best 6.1
Kd 2 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
T-cell
CHEMBL614309
 EC50 8.1 8.1 8.0 1
Protein cereblon/DNA damage-binding protein 1
CHEMBL4630734
 EC50 8.05 8.05 9.0 1
PBMC
CHEMBL613107
 IC50 7.89 7.89 13.0 2
Zinc finger protein Aiolos
CHEMBL4739707
 EC50 7.7 7.7 20.0 1
Unchecked
CHEMBL612545
 IC50 7.68 6.6275 20.8 8
Protein cereblon/Aiolos
CHEMBL4296167
 EC50 7.66 7.66 22.0 1
MM1.S
CHEMBL4296471
 IC50 7.66 6.87 21.9 2
Cereblon/Ikaros
CHEMBL4296103
 EC50 7.62 7.62 24.0 1
Homo sapiens
CHEMBL372
 IC50 7.6 7.6 25.0 1
Unchecked
CHEMBL612545
 EC50 7.57 7.57 27.0 1
NON-PROTEIN TARGET
CHEMBL3879801
 IC50 7.52 7.52 30.0 1
Tumor necrosis factor
CHEMBL1825
 IC50 7.48 7.48 33.0 1
Interleukin-1 beta
CHEMBL1909490
 IC50 7.33 7.33 47.0 1
Protein cereblon/DNA damage-binding protein 1
CHEMBL4630734
 IC50 7.2 6.8 63.1 2
Protein cereblon
CHEMBL3763008
 IC50 7.08 5.722 83.0 5
Protein cereblon
CHEMBL3763008
 Kd 6.8 6.8 157.0 1
Unchecked
CHEMBL612545
 Kd 6.8 6.8 157.0 1
TMD8
CHEMBL4296503
 IC50 6.73 6.73 187.0 1
ADMET
CHEMBL612558
 IC50 6.64 6.64 230.0 1
Cereblon isoform 4
CHEMBL3763007
 Ki 6.1 6.1 800.0 1
OCI-Ly10
CHEMBL4483285
 IC50 5.85 5.85 1400.0 1
JeKo-1
CHEMBL4296445
 IC50 5.58 5.58 2617.3 1
Glyceraldehyde-3-phosphate dehydrogenase, cytosolic
CHEMBL4137
 IC50 5.54 5.54 2900.0 1
Protein cereblon
CHEMBL3763008
 Ki 5.48 5.24 3300.0 2
MCF7
CHEMBL387
 IC50 4.77 4.77 17000.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 410.0 % Homo sapiens
Fu 0.9 - Homo sapiens
T1/2 2.333 hr Homo sapiens
T1/2 3.1 hr Homo sapiens
T1/2 2.65 hr Homo sapiens
T1/2 3.033 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
T-cell EC50 = 8.0 nM 8.1 Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELI... 23168019
Protein cereblon/DNA damage-binding protein 1 EC50 = 9.0 nM 8.05 Displacement of BODIPY FL thalidomide from 6His-tagged CRBN/DDB1 (unknown origin... 35978691
PBMC IC50 = 13.0 nM 7.89 Inhibition of lipopolysaccharide stimulated TNF-alpha release in human PBMC 10386948
PBMC IC50 = 13.0 nM 7.89 Inhibition of TNF-alpha production in LPS-stimulated human PBMC preincubated for... 23168019
Zinc finger protein Aiolos EC50 = 20.0 nM 7.7 Induction of ePL tagged Aiolos degradation in human DF15 cells incubated for 4 h... 37991844
Unchecked IC50 = 20.8 nM 7.68 Cytotoxicity against human MINO cells incubated for 48 hrs by celltitre glo 2.0 ... 37195170
Protein cereblon/Aiolos EC50 = 22.0 nM 7.66 Induction of cereblon-mediated aiolos degradation in human DF15 cells expressing... 28425720
MM1.S IC50 = 21.93 nM 7.66 Antiproliferative activity against human MM1.S cells assessed as cell viability ... 35635954
Cereblon/Ikaros EC50 = 24.0 nM 7.62 Induction of cereblon-mediated ikaros degradation in human DF15 cells expressing... 28425720
Homo sapiens IC50 = 25.0 nM 7.6 Inhibition of lipopolysaccharide stimulated TNF-alpha release in human whole blo... 10386948
Unchecked EC50 = 27.0 nM 7.57 Induction of CRL4/CRBN ubiquitin ligase-mediated aiolos degradation in human DF1... 28358507
NON-PROTEIN TARGET IC50 = 30.0 nM 7.52 Antiproliferative activity against human NAMALWA cells assessed as inhibition of... 23168019
Unchecked IC50 = 31.0 nM 7.51 cytomteric bead array (CBA) assay: The Fix buffer I was warmed up to 37° C. in a... -
Tumor necrosis factor IC50 = 33.0 nM 7.48 cytomteric bead array (CBA) assay: The Fix buffer I was warmed up to 37° C. in a... -
Unchecked IC50 = 35.0 nM 7.46 Immunomodulatory activity in human MM cells 34974338
Interleukin-1 beta IC50 = 47.0 nM 7.33 cytomteric bead array (CBA) assay: The Fix buffer I was warmed up to 37° C. in a... -
Unchecked IC50 = 59.0 nM 7.23 cytomteric bead array (CBA) assay: The Fix buffer I was warmed up to 37° C. in a... -
Protein cereblon/DNA damage-binding protein 1 IC50 = 63.1 nM 7.2 CRBN-DDB1 ligand-displacement AlphaScreen Assay: A thalidomide competition Alpha... -
Protein cereblon IC50 = 83.0 nM 7.08 Inhibition of CRBN in HEK293 cells using NanoGlo substrate incubated for 2 hrs b... 37195170
Protein cereblon Kd = 157.0 nM 6.8 Binding affinity to CRBN (unknown origin) assessed as dissociation constant by T... 37984298

Literature References

PubMed DOI Target Context # Activities
32130004 10.1021/acs.jmedchem.9b01928 Unchecked 7
34795877 10.1021/acsmedchemlett.1c00475 ADMET 7
37902300 10.1021/acs.jmedchem.3c00851 No relevant target 4
34864331 10.1016/j.ejmech.2021.114012 CDK12/Cyclin K 4
36265914 10.1016/j.bmcl.2022.128972 RAW264.7 3
38518734 10.1016/j.bmc.2024.117673 Protein Aster-A 3
33210536 10.1021/acs.jnatprod.0c00350 Unchecked 3
28425720 10.1021/acs.jmedchem.6b01921 Cereblon/Ikaros 3
28425720 10.1021/acs.jmedchem.6b01921 Protein cereblon/Aiolos 3
28358507 10.1021/acs.jmedchem.6b01911 Unchecked 3
36516047 10.1021/acs.jmedchem.2c00739 Histone deacetylase 8 3
27687671 10.1016/j.bmcl.2016.09.009 CDGSH iron-sulfur domain-containing protein 1 2
34364224 10.1016/j.bmc.2021.116331 ADMET 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
34795861 10.1021/acsmedchemlett.1c00368 von Hippel-Lindau disease tumor suppressor/Cyclin-dependent kinase 4 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
34795877 10.1021/acsmedchemlett.1c00475 Cereblon/Ikaros 2
33773263 10.1016/j.ejmech.2021.113353 Unchecked 2
31271281 10.1021/acs.jmedchem.9b00516 Protein cereblon/Histone deacetylase 6 2
10386948 10.1016/s0960-894x(99)00250-4 PBMC 2

Data from ChEMBL 36 via Core Engine