CRBN

Summary

CRBN (cereblon, HGNC:30185) is a protein-coding gene on chromosome 3p26.2, encoding Protein cereblon (Q96SW2). Substrate recognition component of a DCX (DDB1-CUL4-X-box) E3 protein ligase complex that mediates the ubiquitination and subsequent proteasomal degradation of target proteins, such as MEIS2, ILF2 or GLUL. In precision oncology, CRBN Mutation is associated with resistance to Lenalidomide + Pomalidomide in Multiple Myeloma (CIViC Level C).

This gene encodes a protein related to the Lon protease protein family. In rodents and other mammals this gene product is found in the cytoplasm localized with a calcium channel membrane protein, and is thought to play a role in brain development. Mutations in this gene are associated with autosomal recessive nonsyndromic cognitive disability. Multiple transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 51185 — RefSeq curated summary.

At a glance

• Gene–disease (curated): intellectual disability (Moderate, ClinGen) — +2 more curated relationships
• GWAS associations: 13
• Clinical variants (ClinVar): 126 total — 5 pathogenic, 6 likely-pathogenic
• Phenotypes (HPO): 10
• Druggable target: yes — 18 molecules with ChEMBL bioactivity
• Precision-oncology evidence (CIViC): 1 curated variant–drug association
• MANE Select transcript: NM_016302

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:30185
Approved symbol	CRBN
Name	cereblon
Location	3p26.2
Locus type	gene with protein product
Status	Approved
Aliases	MRT2
Ensembl gene	ENSG00000113851
Ensembl biotype	protein_coding
OMIM	609262
Entrez	51185

Gene structure

Transcript identifiers

Ensembl transcripts: 25 — 16 protein_coding, 9 retained_intron

ENST00000231948, ENST00000424814, ENST00000432408, ENST00000450014, ENST00000459840, ENST00000478353, ENST00000480249, ENST00000482844, ENST00000488263, ENST00000491834, ENST00000492178, ENST00000498442, ENST00000498700, ENST00000639284, ENST00000866173, ENST00000866174, ENST00000866175, ENST00000866176, ENST00000866177, ENST00000925599, ENST00000925600, ENST00000925601, ENST00000925602, ENST00000970439, ENST00000970440

RefSeq mRNA: 2 — MANE Select: NM_016302 NM_001173482, NM_016302

CCDS: CCDS2562, CCDS54547

Canonical transcript exons

ENST00000231948 — 11 exons

Exon	Start	End
ENSE00000720924	3154747	3154831
ENSE00003472985	3156219	3156281
ENSE00003507301	3175163	3175269
ENSE00003537389	3150011	3151045
ENSE00003546323	3167634	3167793
ENSE00003548901	3152456	3152587
ENSE00003551349	3172776	3172925
ENSE00003637887	3153960	3154075
ENSE00003660350	3153424	3153488
ENSE00003675249	3174059	3174261
ENSE00003910438	3179621	3179691

Expression profiles

Bgee: expression breadth ubiquitous, 288 present calls, max score 98.11.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 27.7755 / max 789.4488, expressed in 1798 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
40822	27.7755	1798

Top tissues by expression

293 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
calcaneal tendon	UBERON:0003701	98.11	gold quality
Brodmann (1909) area 23	UBERON:0013554	97.48	gold quality
skin of hip	UBERON:0001554	96.56	gold quality
biceps brachii	UBERON:0001507	96.51	gold quality
endothelial cell	CL:0000115	96.50	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	96.50	gold quality
superficial temporal artery	UBERON:0001614	96.36	gold quality
cauda epididymis	UBERON:0004360	96.26	gold quality
middle temporal gyrus	UBERON:0002771	96.22	gold quality
corpus callosum	UBERON:0002336	96.21	gold quality
postcentral gyrus	UBERON:0002581	96.10	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	96.08	gold quality
parietal pleura	UBERON:0002400	96.03	gold quality
superior frontal gyrus	UBERON:0002661	96.00	gold quality
germinal epithelium of ovary	UBERON:0001304	95.85	gold quality
dorsal root ganglion	UBERON:0000044	95.77	gold quality
entorhinal cortex	UBERON:0002728	95.72	gold quality
caput epididymis	UBERON:0004358	95.67	gold quality
upper leg skin	UBERON:0004262	95.59	gold quality
substantia nigra pars compacta	UBERON:0001965	95.51	gold quality
trabecular bone tissue	UBERON:0002483	95.50	gold quality
monocyte	CL:0000576	95.49	gold quality
sural nerve	UBERON:0015488	95.47	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	95.45	gold quality
lateral nuclear group of thalamus	UBERON:0002736	95.44	gold quality
visceral pleura	UBERON:0002401	95.42	gold quality
mononuclear cell	CL:0000842	95.34	gold quality
parietal lobe	UBERON:0001872	95.34	gold quality
seminal vesicle	UBERON:0000998	95.24	gold quality
leukocyte	CL:0000738	95.21	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 2.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	7.37
E-CURD-112	yes	6.74

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): NFE2L2

miRNA regulators (miRDB)

80 targeting CRBN, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-126-5P	100.00	72.71	3180
HSA-MIR-4533	100.00	69.48	2758
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-5696	99.98	72.36	4487
HSA-MIR-485-3P	99.98	70.68	1585
HSA-MIR-539-3P	99.98	70.74	1616
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-23A-3P	99.95	74.24	3163
HSA-MIR-23B-3P	99.95	74.24	3163
HSA-MIR-23C	99.95	73.92	3192
HSA-MIR-559	99.95	72.28	3609
HSA-MIR-548AB	99.95	71.31	3488
HSA-MIR-144-3P	99.94	73.98	2698
HSA-MIR-548A-5P	99.94	71.27	3482
HSA-MIR-548AD-5P	99.94	71.23	3502
HSA-MIR-548AE-5P	99.94	71.23	3502
HSA-MIR-548AK	99.94	71.24	3488
HSA-MIR-548AM-5P	99.94	71.24	3488
HSA-MIR-548AP-5P	99.94	71.14	3489
HSA-MIR-548AQ-5P	99.94	71.34	3426
HSA-MIR-548AR-5P	99.94	71.28	3515
HSA-MIR-548AS-5P	99.94	71.22	3482
HSA-MIR-548AU-5P	99.94	71.24	3488
HSA-MIR-548AY-5P	99.94	71.23	3502
HSA-MIR-548B-5P	99.94	71.23	3502
HSA-MIR-548BB-5P	99.94	71.27	3509
HSA-MIR-548C-5P	99.94	71.24	3488
HSA-MIR-548D-5P	99.94	71.23	3502
HSA-MIR-548H-5P	99.94	71.24	3488
HSA-MIR-548I	99.94	71.25	3481

Literature-anchored findings (GeneRIF, showing 40)

• A nonsense mutation causing a premature stop codon in CRBN was found in a large kindred with mild mental retardation. ATP-dependent degradation of proteins may play a role in memory and learning. (PMID:15557513)
• This may suggest new functions of CRBN in cell nucleolus besides its mitochondria protease activity in cytoplasm. (PMID:17380424)
• Nonsense mutation (R419X) CRBN disturbs the development of adult brain BK(Ca) isoforms. These changes are predicted to result in BK(Ca) channels with a higher intracellular Ca(2+) sensitivity, faster activation, and slower deactivation kinetics. (PMID:18414909)
• The results suggest that mutCRBN may cause ARNSID by disrupting the developmental regulation of BK(Ca) in brain regions that are critical for memory and learning. (PMID:20131966)
• CRBN directly interacts with the alpha1 subunit of AMP-activated protein kinase (AMPK alpha1) and inhibits the activation of AMPK activation. (PMID:21232561)
• CRBN is an essential requirement for immunoregulatory drugs activity and a possible biomarker for the clinical assessment of antimyeloma efficacy. (PMID:21860026)
• Data show that in a cereblon-dependent fashion, lenalidomide downregulates IRF4 and SPIB, transcription factors that together prevent IFNbeta production. (PMID:22698399)
• These findings suggest that CRBN may modulate proteasome activity by directly interacting with the beta7 subunit. (PMID:23026050)
• We conclude that CRBN expression may be associated with the clinical efficacy of thalidomide. (PMID:23233657)
• We investigated the role of CRBN in response to lenalidomide in myelodysplastic syndrome infants without chromosome 5 deletion. (PMID:23434730)
• Findings suggest an approach for the treatment of mental retardation associated with cereblon nonsense mutation. (PMID:23983124)
• CRBN and IRF4 have been shown to be associated with response to lenalidomide in patients, these findings do not translate back to HMCLs, which could be attributable to factors present in the bone marrow microenvironment. (PMID:23992230)
• CRBN expression may provide a biomarker to predict response to Immunomodulatory drugs in patients with MM and its high expression can serve as a marker of good prognosis. (PMID:24118365)
• Data indicate that low cereblon (CRBN) expression can predict resistance to immunomodulatory drug (IMiD monotherapy and is a predictive biomarker for survival outcomes. (PMID:24129344)
• In the three intrinsically IMiD-resistant cell lines that clearly express detectable levels of cereblon, the absence of CRBN and DDB1 mutations suggest that potential cereblon-independent mechanisms of resistance exist (PMID:24166296)
• Presents a molecular model in which drug binding to cereblon results in the interaction of Ikaros and Aiolos to CRL4(CRBN) , leading to their ubiquitination, subsequent proteasomal degradation and T cell activation. (PMID:24328678)
• CRBN expression in bone marrow myeloma cells is associated with superior treatment response to lenalidomide in refractory myeloma and thalidomide/dexamethasone in new patients. CRBN is a crucial factor for the anti-MM effect of immunomodulators. (PMID:24687382)
• Data suggest that cereblon (CRBN) expression in peripheral blood chronic lymphocytic leukemia (CLL) cells is independent of prognostic factors and may be considered a potential biomarker. (PMID:24925210)
• structures of the DDB1-CRBN complex bound to thalidomide, lenalidomide and pomalidomide (PMID:25043012)
• The study presents the crystal structure of human CRBN bound to DDB1 and the drug lenalidomide. (PMID:25108355)
• High levels of full-length CRBN mRNA in lower risk 5q deletion patients are necessary for the efficacy of lenalidomide. (PMID:25284710)
• Studied the protein cereblon , which has been recently indentified as a primary target of thalidomide and its C-terminal part as responsible for binding thalidomide within a domain carrying several invariant cysteine and tryptophan residues. (PMID:25569776)
• A copy number gain of CRBN gene might be responsible for developmental delay/intellectual disability. (PMID:25858704)
• Our data are consistent with the idea that the CUL4A/B-DDB1-CRBN complex catalyses the polyubiquitination and thus controls the degradation of CLC-1 channels. (PMID:26021757)
• Structural dynamics of the cereblon ligand binding domain. (PMID:26024445)
• The anti-PEL effects of IMiDs involved cereblon-dependent suppression of IRF4 and rapid degradation of IKZF1, but not IKZF3. Small hairpin RNA-mediated knockdown of MYC enhanced the cytotoxicity of IMiDs (PMID:26119939)
• dual assay demonstrated superior Cereblon IHC measurement in MM samples compared with the single IHC assay using a published commercial rabbit polyclonal Cereblon antibody and could be used to explore the potential utility of Cereblon as a biomarker in the clinic (PMID:26186254)
• Although abnormal CRBN function may be associated with intellectual disability disease onset, its cellular mechanism is still unclear. Here, we examine the role of CRBN in aggresome formation and cytoprotection. (PMID:26188093)
• GS is acetylated at lysines 11 and 14, yielding a degron that is necessary and sufficient for binding and ubiquitylation by CRL4(CRBN) and degradation by the proteasome. (PMID:26990986)
• These results support the notion that the cereblon binding partner AGO2 plays an important role in regulating MM cell growth and survival and AGO2 could be considered as a novel drug target for overcoming IMiD resistance in MM cells. (PMID:27142104)
• results suggest that CRBN binds to Ikaros via its N-terminal region and regulates transcriptional activities of Ikaros and its downstream target, enkephalin (PMID:27329811)
• 45.2 of multiple myeloma patients were CRBN(+). Among patients treated with thalidomide-based regimens, CRBN(+) patients showed a better treatment response than did CRBN-negative patients. There was no significant difference in survival outcomes between thalidomide- and bortezomib-based regimens in CRBN(+) patients. (PMID:27365142)
• mitochondrially expressed CRBN exhibited protease activity, and was induced by oxidative stress. (PMID:27417535)
• Compared with newly diagnosed multiple myeloma, an increased prevalence of mutations in the Ras pathway genes KRAS, NRAS, and/or BRAF (72%), as well as TP53 (26%), CRBN (12%), and CRBN pathway genes (10%) was observed. (PMID:27458004)
• overview of the current understanding of mechanism of action of Immunomodulatory drugs via CRBN and prospects for the development of new drugs that degrade protein of interest. (PMID:27460676)
• CRBN negatively regulates TLR4 signaling via attenuation of TRAF6 and TAB2 ubiquitination. (PMID:27468689)
• we identify Rabex-5 as a Immunomodulatory drugs (IMiDs) target molecule that functions to restrain TLR activated auto-immune promoting pathways. We propose that release of Rabex-5 from complex with Cereblon enables the suppression of immune responses, contributing to the antiinflammatory properties of IMiDs. (PMID:27601648)
• CRBN expression is of prognostic value in MM patients ineligible for ASCT treated with thalidomide as an immunomodulatory drug. With low expression indicating a possible suboptimal treatment outcome, measurement of CRBN expression might serve as additional prognostic tool in the personalized treatment approach. (PMID:27618360)
• We sequenced CRBN-thalidomide binding region in 38 thalidomide embryopathy individuals and 136 Brazilians without congenital anomalies, and performed in silico analyses. Eight variants were identified, seven intronic and one in 3’UTR. (PMID:27751757)
• High CRBN expression is associated with multiple myeloma. (PMID:28017969)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	crbn	ENSDARG00000054250
mus_musculus	Crbn	ENSMUSG00000005362
rattus_norvegicus	Crbn	ENSRNOG00000006534
drosophila_melanogaster	ohgt	FBGN0037780
caenorhabditis_elegans		WBGENE00010891

Protein

Protein identifiers

Protein cereblon — Q96SW2 (reviewed: Q96SW2)

All UniProt accessions (4): Q96SW2, A0A1W2PPJ5, J3QT51, J3QT87

UniProt curated annotations — full annotation on UniProt →

Function. Substrate recognition component of a DCX (DDB1-CUL4-X-box) E3 protein ligase complex that mediates the ubiquitination and subsequent proteasomal degradation of target proteins, such as MEIS2, ILF2 or GLUL. Normal degradation of key regulatory proteins is required for normal limb outgrowth and expression of the fibroblast growth factor FGF8. Maintains presynaptic glutamate release and consequently cognitive functions, such as memory and learning, by negatively regulating large-conductance calcium-activated potassium (BK) channels in excitatory neurons. Likely to function by regulating the assembly and neuronal surface expression of BK channels via its interaction with KCNT1. May also be involved in regulating anxiety-like behaviors via a BK channel-independent mechanism. Plays a negative role in TLR4 signaling by interacting with TRAF6 and ECSIT, leading to inhibition of ECSIT ubiquitination, an important step of the signaling.

Subunit / interactions. Interacts with KCNT1. Component of a DCX (DDB1-CUL4-X-box) protein ligase complex, at least composed of CRBN, CUL4A, DDB1 and RBX1. Interacts directly with DDB1. Interacts (in pomalidomide-bound form) with IKZF1 and IKZF3. Interacts with ILF2. Interacts with TRAF6 and ECSIT.

Subcellular location. Cytoplasm. Nucleus. Membrane.

Tissue specificity. Widely expressed. Highly expressed in brain.

Post-translational modifications. Ubiquitinated, ubiquitination is mediated by its own DCX protein ligase complex.

Disease relevance. Intellectual developmental disorder, autosomal recessive 2 (MRT2) [MIM:607417] A disorder characterized by significantly below average general intellectual functioning associated with impairments in adaptive behavior and manifested during the developmental period. MRT2 patients display mild intellectual disability with a standard IQ ranged from 50 to 70. IQ scores are lower in males than females. Developmental milestones are mildly delayed. There are no dysmorphic or autistic features. The disease is caused by variants affecting the gene represented in this entry.

Domain organisation. The CULT domain binds thalidomide and related drugs, such as pomalidomide and lenalidomide. Drug binding leads to a change in substrate specificity of the human DCX (DDB1-CUL4-X-box) E3 protein ligase complex, while no such change is observed in rodents.

Pathway. Protein modification; protein ubiquitination.

Miscellaneous. Thalidomide was widely prescribed to pregnant women in the late 1950s as a sedative and as treatment against morning sickness. Thalidomide was found to be teratogenic, causing multiple birth defects. More recently, thalidomide use has increased for the treatment of multiple myeloma and erythema nodosum leprosum, a painful complication of leprosy. Binding of pomalidomide and other thalidomide-related drugs leads to a change in substrate specificity of the human DCX (DDB1-CUL4-X-box) E3 protein ligase complex, and this is probably the underlying cause of the teratogenic activity of thalidomide, possibly due to abnormal regulation of the BMP and FGF8 signaling pathways. The thalidomide-induced change in substrate specificity leads to decreased degradation of MEIS2 and other target proteins and increased degradation of MYC, IRF4, IKZF1 and IKZF3, and this is probably the reason for the anti-proliferative and immunomodulatory effects of thalidomide and related drugs. Thalidomide is also teratogenic in chicken and zebrafish, but not in mice.

Similarity. Belongs to the CRBN family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q96SW2-1	1	yes
Q96SW2-2	2

RefSeq proteins (2): NP_001166953, NP_057386* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR003111	Lon_prtase_N	Domain
IPR004910	Yippee/Mis18/Cereblon	Domain
IPR015947	PUA-like_sf	Homologous_superfamily
IPR034750	CULT	Domain
IPR046336	Lon_prtase_N_sf	Homologous_superfamily

Pfam: PF02190, PF03226

UniProt features (66 total): strand 22, helix 16, binding site 7, turn 6, sequence conflict 4, mutagenesis site 3, domain 2, chain 1, modified residue 1, splice variant 1, sequence variant 1, region of interest 1, compositionally biased region 1

Structure

Experimental structures (PDB)

90 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
4M91	X-RAY DIFFRACTION	1.1
9CUO	X-RAY DIFFRACTION	1.6
9OHQ	X-RAY DIFFRACTION	1.6
9DOM	X-RAY DIFFRACTION	1.69
7BQV	X-RAY DIFFRACTION	1.8
9O91	X-RAY DIFFRACTION	1.86
7BQU	X-RAY DIFFRACTION	1.9
9GAO	X-RAY DIFFRACTION	1.95
9FJX	X-RAY DIFFRACTION	2
8RQC	X-RAY DIFFRACTION	2.15
8RQ8	X-RAY DIFFRACTION	2.19
9OHR	X-RAY DIFFRACTION	2.34
9SFM	X-RAY DIFFRACTION	2.39
8TNQ	ELECTRON MICROSCOPY	2.41
9ODR	X-RAY DIFFRACTION	2.42
5FQD	X-RAY DIFFRACTION	2.45
8OIZ	X-RAY DIFFRACTION	2.5
8RQA	X-RAY DIFFRACTION	2.5
8TNR	ELECTRON MICROSCOPY	2.5
9GY3	X-RAY DIFFRACTION	2.5
9OS2	ELECTRON MICROSCOPY	2.5
9SAF	ELECTRON MICROSCOPY	2.55
11MR	ELECTRON MICROSCOPY	2.6
9ODS	X-RAY DIFFRACTION	2.61
9SAI	ELECTRON MICROSCOPY	2.66
9OUK	ELECTRON MICROSCOPY	2.69
9NWS	ELECTRON MICROSCOPY	2.7
9NWT	ELECTRON MICROSCOPY	2.7
8OJH	X-RAY DIFFRACTION	2.72
9D0X	ELECTRON MICROSCOPY	2.84

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q96SW2-F1	86.87	0.72

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Ligand- & substrate-binding residues (7): 391; 394; 323; 326; 378; 380; 386

Post-translational modifications (1): 25

Mutagenesis-validated functional residues (3):

Position	Phenotype
384	abolishes thalidomide-binding without affecting dcx protein ligase complex activity; when associated with a-386.
386	abolishes thalidomide-binding without affecting dcx protein ligase complex activity; when associated with a-384. abolish
419–442	fails to rescue increased bk channel activity and decreased probability of neurotransmission in a mouse hippocampal neur

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

ID	Pathway
R-HSA-9679191	Potential therapeutics for SARS

MSigDB gene sets: 222 (showing top): GSE45365_CD8A_DC_VS_CD11B_DC_IFNAR_KO_UP, GOBP_NEGATIVE_REGULATION_OF_PROTEIN_CONTAINING_COMPLEX_ASSEMBLY, GOBP_NEGATIVE_REGULATION_OF_TRANSMEMBRANE_TRANSPORT, GOBP_BEHAVIOR, GOBP_MACROMOLECULE_CATABOLIC_PROCESS, GOBP_REGULATION_OF_WNT_SIGNALING_PATHWAY, GOBP_REGULATION_OF_CELLULAR_COMPONENT_BIOGENESIS, GOBP_NEGATIVE_REGULATION_OF_CELLULAR_COMPONENT_ORGANIZATION, GOBP_POSITIVE_REGULATION_OF_CELLULAR_COMPONENT_BIOGENESIS, GOBP_NEGATIVE_REGULATION_OF_TRANSPORT, MILI_PSEUDOPODIA_HAPTOTAXIS_UP, MODULE_480, GOBP_APPENDAGE_DEVELOPMENT, GOBP_REGULATION_OF_PROTEIN_CONTAINING_COMPLEX_ASSEMBLY, GOBP_POST_TRANSLATIONAL_PROTEIN_MODIFICATION

GO Biological Process (8): protein ubiquitination (GO:0016567), positive regulation of Wnt signaling pathway (GO:0030177), negative regulation of protein-containing complex assembly (GO:0031333), positive regulation of protein-containing complex assembly (GO:0031334), negative regulation of monoatomic ion transmembrane transport (GO:0034766), locomotory exploration behavior (GO:0035641), proteasome-mediated ubiquitin-dependent protein catabolic process (GO:0043161), limb development (GO:0060173)

GO Molecular Function (3): transmembrane transporter binding (GO:0044325), metal ion binding (GO:0046872), protein binding (GO:0005515)

GO Cellular Component (6): nucleus (GO:0005634), cytoplasm (GO:0005737), cytosol (GO:0005829), membrane (GO:0016020), Cul4A-RING E3 ubiquitin ligase complex (GO:0031464), perinuclear region of cytoplasm (GO:0048471)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
SARS-CoV Infections	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	4
regulation of protein-containing complex assembly	2
protein-containing complex assembly	2
cytoplasm	2
protein modification by small protein conjugation	1
positive regulation of signal transduction	1
Wnt signaling pathway	1
regulation of Wnt signaling pathway	1
negative regulation of cellular component organization	1
positive regulation of cellular component biogenesis	1
positive regulation of cellular component organization	1
monoatomic ion transmembrane transport	1
negative regulation of transmembrane transport	1
regulation of monoatomic ion transmembrane transport	1
negative regulation of monoatomic ion transport	1
locomotory behavior	1
exploration behavior	1
ubiquitin-dependent protein catabolic process	1
proteasomal protein catabolic process	1
appendage development	1
protein binding	1
cation binding	1
binding	1
intracellular membrane-bounded organelle	1
intracellular anatomical structure	1
Cul4-RING E3 ubiquitin ligase complex	1

Protein interactions and networks

STRING

1662 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CRBN	CUL4A	Q13619	999
CRBN	DDB1	Q16531	999
CRBN	RBX1	P62877	998
CRBN	IKZF1	Q13422	997
CRBN	IKZF3	Q9UKT9	997
CRBN	CUL4B	Q13620	992
CRBN	KCNMA1	Q12791	888
CRBN	CSNK1A1	P48729	885
CRBN	GSPT1	P15170	878
CRBN	LONP2	Q86WA8	855
CRBN	PRSS12	P56730	846
CRBN	BTK	Q06187	836
CRBN	LONP1	P36776	827
CRBN	CC2D1A	Q6P1N0	802
CRBN	BRD4	O60885	795

IntAct

68 interactions, top by confidence:

A	B	Type	Score
CUL4B	COPS2	psi-mi:“MI:0914”(association)	0.790
COPS6	RHOBTB1	psi-mi:“MI:0914”(association)	0.730
CRBN	DDB1	psi-mi:“MI:0915”(physical association)	0.720
PAK5	CRBN	psi-mi:“MI:0915”(physical association)	0.670
CRBN	PAK5	psi-mi:“MI:0915”(physical association)	0.670
CRBN	CUL4A	psi-mi:“MI:0914”(association)	0.650
CRBN	CSNK1A1	psi-mi:“MI:0914”(association)	0.640
CRBN	CSNK1A1	psi-mi:“MI:0915”(physical association)	0.640
CUL4A	COPS2	psi-mi:“MI:0914”(association)	0.640
TGIF2LY	PGP	psi-mi:“MI:0914”(association)	0.640
RBPMS	CRBN	psi-mi:“MI:0915”(physical association)	0.560
MISP	CRBN	psi-mi:“MI:0915”(physical association)	0.560
CRBN		psi-mi:“MI:0915”(physical association)	0.560
CRBN	PMP22	psi-mi:“MI:0915”(physical association)	0.560
KLF11	CRBN	psi-mi:“MI:0915”(physical association)	0.560
COL26A1	CRBN	psi-mi:“MI:0915”(physical association)	0.560

BioGRID (471): CRBN (Two-hybrid), PAK7 (Two-hybrid), CLCN1 (Affinity Capture-Western), CRBN (Two-hybrid), CRBN (Two-hybrid), CRBN (Two-hybrid), CUL4A (Affinity Capture-Western), DDB1 (Affinity Capture-Western), CRBN (Affinity Capture-Western), DDB1 (Affinity Capture-Western), CUL4A (Affinity Capture-Western), CRBN (Affinity Capture-MS), CRBN (Affinity Capture-MS), CRBN (Affinity Capture-MS), CRBN (Affinity Capture-MS)

ESM2 similar proteins: A0JM23, A7E2V1, D2HRF1, E1BVR9, F1ND48, F6Y9J3, O02697, O94952, P0CF65, P0CI65, P42338, P48736, Q32PJ3, Q32PY6, Q3U3W5, Q3UMR0, Q4R3W5, Q4R6Y8, Q56AP7, Q5R5S1, Q5R6Y2, Q5R9R1, Q5REW9, Q5T8I9, Q5U2X1, Q5U2Z5, Q6AZT7, Q6P2P2, Q6P3K3, Q7TNH6, Q7Z494, Q80V94, Q8BGG7, Q8BK06, Q8BTI9, Q8C7D2, Q8CAE2, Q8CD92, Q8NEC7, Q8TF42

Diamond homologs: P0CF65, Q0P564, Q56AP7, Q5R6Y2, Q640S2, Q68EH9, Q8C7D2, Q96SW2

SIGNOR signaling

12 interactions.

A	Effect	B	Mechanism
2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione	“up-regulates activity”	CRBN	“chemical activation”
CRBN	“form complex”	Cullin4-RBX1-DDB1	binding
lenalidomide	“up-regulates activity”	CRBN	“chemical activation”
pomalidomide	“down-regulates activity”	CRBN	“chemical inhibition”
lenalidomide	“down-regulates activity”	CRBN	“chemical inhibition”
CRBN	“down-regulates quantity by destabilization”	SALL4	ubiquitination
thalidomide	“down-regulates activity”	CRBN	“chemical inhibition”
CRBN	“down-regulates quantity by destabilization”	SALL4	binding
CRBN	“down-regulates quantity by destabilization”	TP63	polyubiquitination
FBXO7	“down-regulates quantity by destabilization”	CRBN	binding
“Cullin 1-RBX1-Skp1”	“down-regulates quantity by destabilization”	CRBN	polyubiquitination
CRBN	“down-regulates quantity by destabilization”	IKZF3	ubiquitination

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 49 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
DNA Damage Recognition in GG-NER	7	60.6×	4e-09
Formation of TC-NER Pre-Incision Complex	7	44.9×	2e-08
Neddylation	8	11.5×	3e-05

GO biological processes:

GO term	Partners	Fold	FDR
cellular response to UV	5	34.4×	8e-05
DNA damage response	6	7.5×	9e-03

Disease & clinical

Cancer significance

Clinical variants and AI predictions

ClinVar

126 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	5
Likely pathogenic	6
Uncertain significance	74
Likely benign	17
Benign	9

Top pathogenic / likely-pathogenic (11)

Variant ID	HGVS	Classification
1032731	NM_016302.4(CRBN):c.433C>T (p.Arg145Ter)	Pathogenic
1321315	NM_016302.4(CRBN):c.129dup (p.Pro44fs)	Pathogenic
4071608	NM_016302.4(CRBN):c.846_847del (p.Tyr282_Arg283delinsTer)	Pathogenic
984705	NM_016302.4(CRBN):c.835+1G>A	Pathogenic
987486	NM_016302.4(CRBN):c.807dup (p.Asp270fs)	Pathogenic
1180660	NM_016302.4(CRBN):c.913_914dup (p.Gln306fs)	Likely pathogenic
1196420	NM_016302.4(CRBN):c.235C>T (p.Gln79Ter)	Likely pathogenic
1684148	NM_016302.4(CRBN):c.791G>A (p.Trp264Ter)	Likely pathogenic
1690413	NM_016302.4(CRBN):c.124A>T (p.Lys42Ter)	Likely pathogenic
800320	NM_016302.4(CRBN):c.1100A>T (p.Asn367Ile)	Likely pathogenic
816985	NM_016302.4(CRBN):c.641C>G (p.Ser214Ter)	Likely pathogenic

SpliceAI

2982 predictions. Top by Δscore:

Variant	Effect	Δscore
3:3146532:GATT:G	donor_gain	1.0000
3:3151043:TAC:T	acceptor_gain	1.0000
3:3151046:CTAAG:C	acceptor_loss	1.0000
3:3153418:CCTTA:C	donor_loss	1.0000
3:3153419:CTTA:C	donor_loss	1.0000
3:3153420:TTA:T	donor_loss	1.0000
3:3153484:GTACA:G	acceptor_gain	1.0000
3:3153485:TACA:T	acceptor_gain	1.0000
3:3153486:ACA:A	acceptor_gain	1.0000
3:3153487:CA:C	acceptor_gain	1.0000
3:3153487:CAC:C	acceptor_gain	1.0000
3:3153488:AC:A	acceptor_loss	1.0000
3:3153489:C:CC	acceptor_gain	1.0000
3:3153489:C:T	acceptor_loss	1.0000
3:3153958:A:AC	donor_gain	1.0000
3:3153959:C:CC	donor_gain	1.0000
3:3167633:CCTT:C	donor_gain	1.0000
3:3167792:TT:T	acceptor_gain	1.0000
3:3167794:C:CC	acceptor_gain	1.0000
3:3167794:CTAAA:C	acceptor_loss	1.0000
3:3172770:TCTTA:T	donor_loss	1.0000
3:3172771:CTTA:C	donor_loss	1.0000
3:3172772:TTA:T	donor_loss	1.0000
3:3172773:TA:T	donor_loss	1.0000
3:3172774:A:AC	donor_gain	1.0000
3:3172774:A:AG	donor_loss	1.0000
3:3172775:C:CC	donor_gain	1.0000
3:3172775:CCCAT:C	donor_gain	1.0000
3:3172779:T:C	donor_gain	1.0000
3:3172795:G:C	donor_gain	1.0000

AlphaMissense

2926 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
3:3150988:A:C	F402L	1.000
3:3150988:A:T	F402L	1.000
3:3150990:A:G	F402L	1.000
3:3150994:C:A	W400C	1.000
3:3150994:C:G	W400C	1.000
3:3150996:A:G	W400R	1.000
3:3150996:A:T	W400R	1.000
3:3150998:C:T	G399E	1.000
3:3151023:A:G	C391R	1.000
3:3152466:A:G	W380R	1.000
3:3152466:A:T	W380R	1.000
3:3153988:A:G	L308P	1.000
3:3154069:G:A	S281F	1.000
3:3150944:A:G	L417S	0.999
3:3150951:A:G	W415R	0.999
3:3150951:A:T	W415R	0.999
3:3150952:A:C	F414L	0.999
3:3150952:A:T	F414L	0.999
3:3150953:A:G	F414S	0.999
3:3150954:A:G	F414L	0.999
3:3150989:A:G	F402S	0.999
3:3150995:C:G	W400S	0.999
3:3150998:C:A	G399V	0.999
3:3150999:C:G	G399R	0.999
3:3150999:C:T	G399R	0.999
3:3151014:A:G	C394R	0.999
3:3151021:A:C	C391W	0.999
3:3151022:C:G	C391S	0.999
3:3151022:C:T	C391Y	0.999
3:3151023:A:T	C391S	0.999

dbSNP variants (sampled 300 via entrez): RS1000042317 (3:3161373 T>C), RS1000079919 (3:3150141 T>C,G), RS1000102252 (3:3166882 G>C), RS1000229379 (3:3180946 A>C,T), RS1000721359 (3:3163932 T>C), RS1000869085 (3:3168566 A>G,T), RS1000898777 (3:3168310 A>C,G), RS1000905850 (3:3171923 C>T), RS1000961434 (3:3149261 A>ATACTT), RS1000967373 (3:3150267 TTCGTGGGCTCAA>T), RS1001032166 (3:3177198 C>T), RS1001131559 (3:3173213 A>G), RS1001232881 (3:3171338 A>G), RS1001460575 (3:3177010 A>T), RS1001567010 (3:3176604 T>C)

Disease associations

OMIM: gene MIM:609262 | disease phenotypes: MIM:607417, MIM:254500

GenCC curated gene-disease

Disease	Classification	Inheritance
autosomal recessive non-syndromic intellectual disability	Supportive	Autosomal recessive
intellectual disability, autosomal recessive 2	Limited	Autosomal recessive

ClinGen Gene-Disease Validity (1)

Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.

Disease	Classification	Inheritance
intellectual disability	Moderate	AR

Mondo (4): intellectual disability, autosomal recessive 2 (MONDO:0011828), intellectual disability (MONDO:0001071), plasma cell myeloma (MONDO:0009693), autosomal recessive non-syndromic intellectual disability (MONDO:0019502)

Orphanet (4): Autosomal recessive non-syndromic intellectual disability (Orphanet:88616), Multiple myeloma (Orphanet:29073), AL amyloidosis (Orphanet:85443), NON RARE IN EUROPE: Unexplained intellectual disability (Orphanet:319658)

HPO phenotypes

10 total (10 of 10 shown, HPO-id order):

HPO	Term
HP:0000007	Autosomal recessive inheritance
HP:0001250	Seizure
HP:0001256	Mild intellectual disability
HP:0001263	Global developmental delay
HP:0001344	Absent speech
HP:0003593	Infantile onset
HP:0007018	Attention deficit hyperactivity disorder
HP:0010864	Severe intellectual disability
HP:0031936	Delayed ability to walk
HP:0100716	Self-injurious behavior

GWAS associations

13 associations (top):

Study	Trait	p-value
GCST001491_7	Immune response to smallpox vaccine (IL-6)	8.000000e-07
GCST001760_5	White matter integrity	6.000000e-06
GCST002337_146	Amyotrophic lateral sclerosis (sporadic)	4.000000e-06
GCST003820_6	Knee osteoarthritis	8.000000e-06
GCST004618_59	White blood cell count (basophil)	1.000000e-26
GCST004631_58	Basophil percentage of white cells	1.000000e-28
GCST004634_18	Basophil percentage of granulocytes	3.000000e-25
GCST005042_6	Restless legs syndrome	2.000000e-13
GCST005976_14	White blood cell count (basophil)	3.000000e-20
GCST010725_42	Malaria	5.000000e-07
GCST010725_55	Malaria	9.000000e-07
GCST90002379_35	Basophil count	7.000000e-17
GCST90002380_136	Basophil percentage of white cells	2.000000e-17

EFO canonical traits (5, from GWAS)

EFO ID	Trait name
EFO:0004645	response to vaccine
EFO:0004641	white matter integrity
EFO:0005090	basophil count
EFO:0007992	basophil percentage of leukocytes
EFO:0007995	basophil percentage of granulocytes

MeSH disease descriptors (3)

Descriptor	Name	Tree numbers
D008607	Intellectual Disability	C10.597.606.360; C23.888.592.604.646; F01.700.687; F03.625.539
D009101	Multiple Myeloma	C04.557.595.500; C14.907.454.460; C15.378.147.780.650; C15.378.463.515.460; C20.683.515.845; C20.683.780.650
C564404	Mental Retardation, Autosomal Recessive 2 (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (303): CHEMBL3763008 (SINGLE PROTEIN), CHEMBL3833061 (PROTEIN COMPLEX), CHEMBL4296102 (PROTEIN COMPLEX), CHEMBL4296103 (PROTEIN COMPLEX), CHEMBL4296125 (PROTEIN-PROTEIN INTERACTION), CHEMBL4296126 (PROTEIN-PROTEIN INTERACTION), CHEMBL4296127 (PROTEIN-PROTEIN INTERACTION), CHEMBL4296128 (PROTEIN-PROTEIN INTERACTION), CHEMBL4296129 (PROTEIN-PROTEIN INTERACTION), CHEMBL4296130 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

18 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 392,290 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL3137312	DASABUVIR	4	1,088
CHEMBL43452	POMALIDOMIDE	4	13,354
CHEMBL468	THALIDOMIDE	4	97,393
CHEMBL848	LENALIDOMIDE	4	5,256
CHEMBL1171837	PONATINIB	4	8,955
CHEMBL4208229	ASCIMINIB	4	882
CHEMBL3545311	BRIGATINIB	4	5,634
CHEMBL601719	CRIZOTINIB	4	14,403
CHEMBL3989927	IBERDOMIDE	3	1,300
CHEMBL566	URACIL	3	235,501
CHEMBL5095210	VEPDEGESTRANT	3	336
CHEMBL4648616	MEZIGDOMIDE	3	477
CHEMBL3989934	AVADOMIDE	2	1,506
CHEMBL4297376	E-7820	2	476
CHEMBL77517	INDISULAM	2	799
CHEMBL1976040	ADAVOSERTIB	2	1,738
CHEMBL1230609	FORETINIB	2	3,096
CHEMBL4297459	CC-11006	1	96

Clinical evidence (CIViC)

Drug × variant × indication: 1 predictive associations from 1 curated evidence items.

Variant	Therapy	Indication	Effect	Level	CIViC
CRBN Mutation	Lenalidomide + Pomalidomide	Multiple Myeloma	Resistance	CIViC C	EID1766

PharmGKB: 1 entry (VIP=true, CPIC=false)

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs1705814	CRBN		0.00	0

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: enzyme — E3 ubiquitin ligase components

Most potent curated ligand interactions (21 total), top 21:

Ligand	Action	Affinity	Parameter
AK-2292	Binding	9.77	pKi
MG-277	Binding	8.51	pIC50
thalidomide	Binding	8.07	pKd
MD-222	Binding	8.0	pIC50
TL12-186	Binding	7.92	pIC50
SJ995973	Binding	7.77	pIC50
compound 7f [PMID: 31251063]	Binding	7.7	pKi
mezigdomide	Binding	7.52	pIC50
dBRD9	Binding	7.5	pIC50
avadomide	Binding	7.27	pIC50
iberdomide	Binding	7.22	pIC50
dTAG-13	Binding	7.19	pIC50
PTD10	Binding	6.97	pIC50
NVP-DKY709	Binding	6.89	pIC50
SK5527	Binding	5.95	pKi
pomalidomide	Binding	5.92	pIC50
TX-16	Binding	5.85	pKi
lenalidomide	Binding	5.82	pIC50
CBPD-268	Binding	5.74	pIC50
SB-405483	Allosteric modulator	5.6	pKd
MS40	Binding	4.83	pKd

Binding affinities (BindingDB)

998 measured of 1565 human assays (1876 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
3-[4-[[(1R)-1-(4-methoxyphenyl)ethyl]amino]-1,3-dihydroisoindol-2-yl]piperidine-2,6-dione	KD	16 nM	US-20250129041: MOLECULAR GLUE AND USES THEREOF
3-(1-oxo-5-(7-(pyrrolidin-1- ylmethyl)imidazo[1,5-a]pyridin-5- yl)isoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(6-(((2,6-dichloro- phenethyl)amino)methyl)imi- dazo[1,2-a]pyridin-8-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(7-(azetidin-1- ylmethyl)imidazo[1,5-a]pyridin-5- yl)-1-oxoisoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(1-oxo-5-(7-(piperidin-1- ylmethyl)imidazo[1,5-a]pyridin-5- yl)isoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(6-(((2-chloro- phenethyl)amino)methyl)imi- dazo[1,2-a]pyridin-8-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(1-oxo-5-(6-(((1- phenylethyl)amino)methyl)imidazo [1,2-a]pyridin-8-yl)isoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(7-((3-methylpyrrolidin-1- yl)methyl)imidazo[1,5-a]pyridin-5- yl)-1-oxoisoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(1-oxo-5-(6-(((2-phenylpropan- 2-yl)amino)methyl)imidazo[1,2- a]pyridin-8-yl)isoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(1-oxo-5-(6-((2- phenylpyrrolidin-1- yl)methyl)imidazo[1,2-a]pyridin-8- yl)isoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(6-(((2- chlorophenethyl)amino)methyl)-1- methyl-1H-benzo[d]imidazol-4- yl)-1-oxoisoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(7-((diethylamino)methyl) imidazo[1,5-a]pyridin-5-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(7- ((benzylamino)methyl)imidazo[1,5- a]pyridin-5-yl)-1-oxoisoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(1-oxo-5-(7-((((S*)-1- phenylethyl)amino)methyl)imidazo [1,5-a]pyridin-5-yl)isoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(1-methyl-4-(pyrrolidin-1- ylmethyl)-1H-pyrrolo[2,3- b]pyridin-6-yl)-1-oxoisoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(1-methyl-4-(piperidin-1- ylmethyl)-1H-pyrrolo[2,3- b]pyridin-6-yl)-1-oxoisoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(1-oxo-5-(4-(pyrrolidin-1- ylmethyl)-1H-pyrrolo[2,3- b]pyridin-6-yl)isoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(7-(((2- chlorophenethyl)amino)methyl)imi- dazo[1,5-a]pyridin-5-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(1-methyl-4- (thiomorpholinomethyl)-1H- pyrrolo[2,3-b]pyridin-6-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(1-methyl-4-((tetrahydro-1H- furo[3,4-c]pyrrol-5(3H)- yl)methyl)-1H-pyrrolo[2,3- b]pyridin-6-yl)-1-oxoisoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(4-((6-azaspiro[2.5]octan-6- yl)methyl)-1-methyl-1H- pyrrolo[2,3-b]pyridin-6-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(7-((((1-methyl-1H-indol-7- yl)methyl)amino)methyl)imi- dazo[1,5-a]pyridin-5-yl)-1- oxoisoindolin- 2-yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(4-((3,4-dihydroisoquinolin- 2(1H)-yl)methyl)-1-methyl-1H- pyrrolo[2,3-b]pyridin-6-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(1-oxo-5-(7-((2- phenylpyrrolidin-1- yl)methyl)imidazo[1,5-a]pyridin-5- yl)isoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(4-((3- azabicyclo[3.1.0]hexan-3- yl)methyl)-1-methyl-1H- pyrrolo[2,3-b]pyridin-6-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(4-((7-azaspiro[3.5]nonan-7- yl)methyl)-1-methyl-1H- pyrrolo[2,3-b]pyridin-6-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(4-methoxy-1-oxo-5-(7- (pyrrolidin-1- ylmethyl)imidazo[1,5-a]pyridin-5- yl)isoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(1-methyl-4-((2- phenylazetidin-1-yl)methyl)-1H- pyrrolo[2,3-b]pyridin-6-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(7-methoxy-1-oxo-5-(7- (pyrrolidin-1- ylmethyl)imidazo[1,5-a]pyridin-5- yl)isoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(4- ((hexahydrocyclopenta[c]pyrrol- 2(1H)-yl)methyl)-1-methyl-1H- pyrrolo[2,3-b]pyridin-6-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(1-oxo-5-(6-(piperidin-1- ylmethyl)imidazo[1,2-a]pyridin-8- yl)isoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(4-((2-oxa-7- azaspiro[3.5]nonan-7-yl)methyl)-1- methyl-1H-pyrrolo[2,3-b]pyridin- 6-yl)-1-oxoisoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(6-((4,4-difluoropiperidin-1- yl)methyl)imidazo[1,2-a]pyridin-8- yl)-1-oxoisoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(4-fluoro-5-(1-methyl-4- (pyrrolidin-1-ylmethyl)-1H- pyrrolo[2,3-b]pyridin-6-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(6-((4,4-dimethylpiperidin-1- yl)methyl)imidazo[1,2-a]pyridin-8- yl)-1-oxoisoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(6-(((2-chloro- benzyl)amino)methyl)imidazo [1,2-a]pyridin-8-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(1-oxo-5-(4-(pyrrolidin-1- ylmethyl)-5,6,7,8- tetrahydroquinolin-2-yl)isoindolin- 2-yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(6-(((2,4-dichloro- phenethyl)amino)methyl)imi- dazo[1,2-a]pyridin-8-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(1-oxo-5-(4-(pyrrolidin-1- ylmethyl)-6,7-dihydro-5H- cyclopenta[b]pyridin-2- yl)isoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(1-oxo-5-(4-(pyrrolidin-1- ylmethyl)-1-(tetrahydro-2H-pyran- 4-yl)-1H-pyrrolo[2,3-b]pyridin-6- yl)isoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(4-((3-methoxyazetidin-1- yl)methyl)-1-methyl-1H- pyrrolo[2,3-b]pyridin-6-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(1-methyl-4-(1-(pyrrolidin-1- yl)ethyl)-1H-pyrrolo[2,3-b]pyridin- 6-yl)-1-oxoisoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(1-methyl-4-((4- (trifluoromethyl)piperidin-1- yl)methyl)-1H-pyrrolo[2,3- b]pyridin-6-yl)-1-oxoisoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(4-((3-methoxypyrrolidin-1- yl)methyl)-1-methyl-1H- pyrrolo[2,3-b]pyridin-6-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(1-(oxetan-3-yl)-4- ((tetrahydro-1H-furo[3,4-c]pyrrol- 5(3H)-yl)methyl)-1H-pyrrolo[2,3- b]pyridin-6-yl)-1-oxoisoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(4-((4-fluoropiperidin-1- yl)methyl)-1-(oxetan-3-yl)-1H- pyrrolo[2,3-b]pyridin-6-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(4-((hexahydropyrrolo[1,2- a]pyrazin-2(1H)-yl)methyl)-1- methyl-1H-pyrrolo[2,3-b]pyridin- 6-yl)-1-oxoisoindolin-2- yl)piperidine-2,6-dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(4-((3- (hydroxymethyl)pyrrolidin-1- yl)methyl)-1-methyl-1H- pyrrolo[2,3-b]pyridin-6-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(4-((4-methoxypiperidin-1- yl)methyl)-1-(oxetan-3-yl)-1H- pyrrolo[2,3-b]pyridin-6-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS
3-(5-(4-((4- (dimethylamino)piperidin-1- yl)methyl)-1-(oxetan-3-yl)-1H- pyrrolo[2,3-b]pyridin-6-yl)-1- oxoisoindolin-2-yl)piperidine-2,6- dione	IC50	20 nM	US-20250214991: BICYCLIC HETEROARYL-CONTAINING COMPOUNDS AS IKZF2 DEGRADERS

ChEMBL bioactivities

1297 potent at pChembl≥5 of 1585 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.73	EC50	0.0187	nM	CHEMBL5076100
10.70	IC50	0.02	nM	CHEMBL5090416
10.66	EC50	0.022	nM	CHEMBL5414378
10.62	EC50	0.0238	nM	CHEMBL5207946
10.56	EC50	0.0276	nM	CHEMBL5200341
10.15	EC50	0.0714	nM	CHEMBL5193611
10.00	EC50	0.1	nM	CHEMBL4645677
10.00	EC50	0.1	nM	CHEMBL4640365
10.00	EC50	0.1	nM	CHEMBL4638224
10.00	EC50	0.1	nM	CHEMBL4636670
10.00	EC50	0.1	nM	CHEMBL4647905
10.00	EC50	0.1	nM	CHEMBL4647587
10.00	EC50	0.1	nM	CHEMBL4637801
10.00	EC50	0.1	nM	CHEMBL4645982
10.00	EC50	0.1	nM	CHEMBL4636184
10.00	EC50	0.1	nM	CHEMBL4644660
10.00	EC50	0.1	nM	CHEMBL4637622
10.00	EC50	0.1	nM	CHEMBL4879244
10.00	EC50	0.1	nM	CHEMBL5094191
9.96	Kd	0.11	nM	CHEMBL4748640
9.89	Kd	0.13	nM	CHEMBL4742867
9.85	Kd	0.14	nM	CHEMBL5561819
9.70	EC50	0.2	nM	CHEMBL4641034
9.70	EC50	0.2	nM	CHEMBL4642904
9.70	EC50	0.2	nM	CHEMBL4741262
9.70	EC50	0.2	nM	CHEMBL4747369
9.66	Kd	0.22	nM	CHEMBL5563992
9.64	Kd	0.23	nM	CHEMBL4747034
9.61	IC50	0.244	nM	CHEMBL5178566
9.59	Kd	0.26	nM	CHEMBL4747034
9.55	Kd	0.28	nM	CHEMBL4748640
9.52	EC50	0.3	nM	CHEMBL4645692
9.52	EC50	0.3	nM	CHEMBL4642197
9.52	EC50	0.3	nM	CHEMBL4646021
9.52	EC50	0.3	nM	CHEMBL4648954
9.52	EC50	0.3	nM	CHEMBL4877348
9.52	IC50	0.3	nM	CHEMBL6133093
9.51	IC50	0.31	nM	CHEMBL4744617
9.49	Kd	0.32	nM	CHEMBL4642168
9.47	Kd	0.34	nM	CHEMBL5561261
9.43	Kd	0.37	nM	CHEMBL5567457
9.42	Kd	0.38	nM	CHEMBL4742867
9.42	Kd	0.38	nM	CHEMBL5567766
9.40	EC50	0.4	nM	CHEMBL4642361
9.40	EC50	0.4	nM	CHEMBL4639846
9.40	IC50	0.4	nM	CHEMBL4760508
9.40	IC50	0.4	nM	CHEMBL4745409
9.40	IC50	0.4	nM	CHEMBL4800591
9.40	IC50	0.4	nM	CHEMBL4745755
9.40	IC50	0.4	nM	CHEMBL4754618

PubChem BioAssay actives

389 with measured affinity, of 6100 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
N-[4-[4-[4-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]piperazine-1-carbonyl]piperidin-1-yl]phenyl]-2-phenoxypyrimidine-5-carboxamide	1858479: PROTAC activity at CRBN/H-PGDS in human KU812 cells assessed as reduction in H-PGDS levels incubated for 24 hrs by Western blotting analysis	ec50	<0.0001	uM
4-[[4-[1-[3-(cyanomethyl)-1-ethylsulfonylazetidin-3-yl]pyrazol-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-N-[3-[4-[4-(2,6-dioxopiperidin-3-yl)phenyl]piperazin-1-yl]propyl]benzamide	1827294: Binding affinity to CRBN (unknown origin) measured by Fluorescent Polarization assay	ic50	<0.0001	uM
N-[4-[4-[4-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]piperazine-1-carbonyl]piperidin-1-yl]phenyl]-2-phenoxypyrimidine-5-carboxamide	1858479: PROTAC activity at CRBN/H-PGDS in human KU812 cells assessed as reduction in H-PGDS levels incubated for 24 hrs by Western blotting analysis	ec50	<0.0001	uM
N-[4-[4-[4-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]piperazine-1-carbonyl]piperidin-1-yl]phenyl]-4-(1-methylpyrrole-2-carbonyl)piperazine-1-carboxamide	1858479: PROTAC activity at CRBN/H-PGDS in human KU812 cells assessed as reduction in H-PGDS levels incubated for 24 hrs by Western blotting analysis	ec50	<0.0001	uM
2-[2-[2-[2-[2-[2-[6-[4-[3-[3-cyano-4-(2,4-dichloro-5-methoxyanilino)-6-methoxyquinolin-7-yl]oxypropyl]piperazin-1-yl]hexoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]-N-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]acetamide	1678549: Protac binding affinity at CRBN/BCR-ABL (unknown origin) assessed as binding to phosphorylated c-ABL kinase domain by Kinomescan assay	kd	0.0001	uM
2-[2-[6-[4-[3-[3-cyano-4-(2,4-dichloro-5-methoxyanilino)-6-methoxyquinolin-7-yl]oxypropyl]piperazin-1-yl]hexoxy]ethoxy]-N-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]acetamide	1678549: Protac binding affinity at CRBN/BCR-ABL (unknown origin) assessed as binding to phosphorylated c-ABL kinase domain by Kinomescan assay	kd	0.0001	uM
4-[4-[[4-[[2-(2,6-dioxopiperidin-3-yl)-1-oxo-3H-isoindol-4-yl]oxymethyl]phenyl]methyl]piperazin-1-yl]-3-fluorobenzonitrile	1667517: Induction of CRBN-mediated pLOC-ePL-tagged aiolos (unknown origin) degradation in human DF15 cells assessed as minimum protein remaining incubated for 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay	ec50	0.0001	uM
N-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]-2-(trifluoromethoxy)benzenesulfonamide	1814549: PROTAC activity at human CRBN/HiBiT-fused GSPT1 transfected in HEK293T cells assessed as induction of GSPT1 degradation measured after 4 hrs by Nano-Glo HiBiT lytic assay	ec50	0.0001	uM
3-[7-[[4-[[4-(3-fluorophenyl)piperazin-1-yl]methyl]phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1667517: Induction of CRBN-mediated pLOC-ePL-tagged aiolos (unknown origin) degradation in human DF15 cells assessed as minimum protein remaining incubated for 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay	ec50	0.0001	uM
3-[7-[[4-[4-(2,4-dichlorophenyl)piperazine-1-carbonyl]phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1667517: Induction of CRBN-mediated pLOC-ePL-tagged aiolos (unknown origin) degradation in human DF15 cells assessed as minimum protein remaining incubated for 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay	ec50	0.0001	uM
3-[7-[[4-[[4-(4-chlorophenyl)piperazin-1-yl]methyl]phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1667517: Induction of CRBN-mediated pLOC-ePL-tagged aiolos (unknown origin) degradation in human DF15 cells assessed as minimum protein remaining incubated for 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay	ec50	0.0001	uM
3-[7-[[4-[4-(2,4-difluorophenyl)piperazine-1-carbonyl]phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1667517: Induction of CRBN-mediated pLOC-ePL-tagged aiolos (unknown origin) degradation in human DF15 cells assessed as minimum protein remaining incubated for 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay	ec50	0.0001	uM
3-[7-[[4-[4-(4-chlorophenyl)piperazine-1-carbonyl]phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1667517: Induction of CRBN-mediated pLOC-ePL-tagged aiolos (unknown origin) degradation in human DF15 cells assessed as minimum protein remaining incubated for 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay	ec50	0.0001	uM
(3S)-3-[7-[[4-[[4-(2,4-difluorophenyl)piperazin-1-yl]methyl]phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1667517: Induction of CRBN-mediated pLOC-ePL-tagged aiolos (unknown origin) degradation in human DF15 cells assessed as minimum protein remaining incubated for 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay	ec50	0.0001	uM
N-[4-[4-[4-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]piperazine-1-carbonyl]piperidin-1-yl]phenyl]-4-(1-methylpyrrole-2-carbonyl)piperazine-1-carboxamide	1858479: PROTAC activity at CRBN/H-PGDS in human KU812 cells assessed as reduction in H-PGDS levels incubated for 24 hrs by Western blotting analysis	ec50	0.0001	uM
N-(2-chloro-6-methylphenyl)-2-[[6-[4-[6-[2-[2-[2-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]-2-oxoethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]hexyl]piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide	1678549: Protac binding affinity at CRBN/BCR-ABL (unknown origin) assessed as binding to phosphorylated c-ABL kinase domain by Kinomescan assay	kd	0.0002	uM
N-[4-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]butyl]-4-[[4-(1-propylpyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]benzamide	1710172: PROTAC activity at CRBN/JAK2 in human MHHCALL4 cells assessed as protein degradation by immunoblot analysis	ec50	0.0002	uM
3-[7-[[4-[[4-(2-fluorophenyl)piperazin-1-yl]methyl]phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1667517: Induction of CRBN-mediated pLOC-ePL-tagged aiolos (unknown origin) degradation in human DF15 cells assessed as minimum protein remaining incubated for 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay	ec50	0.0002	uM
3-[7-[[4-[[4-(2,4-dichlorophenyl)piperazin-1-yl]methyl]phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1667517: Induction of CRBN-mediated pLOC-ePL-tagged aiolos (unknown origin) degradation in human DF15 cells assessed as minimum protein remaining incubated for 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay	ec50	0.0002	uM
(4S)-1-[4-[4-[3-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]propanoyl]piperazin-1-yl]phenyl]-7,8-dimethoxy-N,4-dimethyl-4,5-dihydro-2,3-benzodiazepine-3-carboxamide	1852448: Protac activity at His-tagged CRBN/FLAG-tagged DDB1 (unknown origin) in presence of Cy5-labeled thalidomide incubated for 60 min by TR-FRET assay	ic50	0.0002	uM
N-(2-chloro-6-methylphenyl)-2-[[6-[4-[6-[2-[2-[6-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]-6-oxohexoxy]ethoxy]ethoxy]hexyl]piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide	1678549: Protac binding affinity at CRBN/BCR-ABL (unknown origin) assessed as binding to phosphorylated c-ABL kinase domain by Kinomescan assay	kd	0.0003	uM
4-[[4-[1-[3-(cyanomethyl)-1-ethylsulfonylazetidin-3-yl]pyrazol-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-N-[2-[4-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]piperazin-1-yl]ethyl]benzamide	1827294: Binding affinity to CRBN (unknown origin) measured by Fluorescent Polarization assay	ic50	0.0003	uM
3-[7-[[4-[[4-(2,6-difluorophenyl)piperazin-1-yl]methyl]phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1667517: Induction of CRBN-mediated pLOC-ePL-tagged aiolos (unknown origin) degradation in human DF15 cells assessed as minimum protein remaining incubated for 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay	ec50	0.0003	uM
3-[7-[[4-[4-(4-fluorophenyl)piperazine-1-carbonyl]phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1667517: Induction of CRBN-mediated pLOC-ePL-tagged aiolos (unknown origin) degradation in human DF15 cells assessed as minimum protein remaining incubated for 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay	ec50	0.0003	uM
N-[2-[4-[[3-[3-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]cyclobutyl]oxypropyl-methylamino]methyl]cyclohexyl]-6-(2-hydroxypropan-2-yl)indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide	2085323: Binding affinity to CRBN/IRAK4 in human OCI-Ly10 cells assessed as dissociation constant by DiscoverX Kd Elect assay	kd	0.0003	uM
(1R,9S,12S,15R,16E,18R,19S,21R,23S,24E,26E,28E,30S,32S,35R)-12-[(2S)-1-[(1S,3R,4R)-4-[2-[[1-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethyl]triazol-4-yl]methoxy]ethoxy]-3-methoxycyclohexyl]propan-2-yl]-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone	1849962: PROTAC activity at CRBN/FKBP12 in human Jurkat cells assessed as induction of FKBP12 degradation incubated for 12 hrs by Western blot analysis	ec50	0.0003	uM
N-[2-[4-(hydroxymethyl)cyclohexyl]-6-(2-hydroxypropan-2-yl)indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide	2085323: Binding affinity to CRBN/IRAK4 in human OCI-Ly10 cells assessed as dissociation constant by DiscoverX Kd Elect assay	kd	0.0004	uM
3-[6-[9-[2-[1-[5-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyrimidin-2-yl]piperidin-4-yl]ethyl]-3,9-diazaspiro[5.5]undecan-3-yl]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1678557: Protac activity at CRBN/ERalpha in human MCF7 cells assessed as induction of ERalpha protein degradation incubated for 8 to 22 hrs by immunofluorescence assay	ic50	0.0004	uM
3-[6-[2-[[7-[5-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyrimidin-2-yl]-7-azaspiro[3.5]nonan-2-yl]methyl]-2,7-diazaspiro[3.5]nonan-7-yl]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1678557: Protac activity at CRBN/ERalpha in human MCF7 cells assessed as induction of ERalpha protein degradation incubated for 8 to 22 hrs by immunofluorescence assay	ic50	0.0004	uM
3-[6-[10-[[1-[5-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyrimidin-2-yl]piperidin-4-yl]methyl]-7-oxa-3,10-diazaspiro[5.6]dodecan-3-yl]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1678557: Protac activity at CRBN/ERalpha in human MCF7 cells assessed as induction of ERalpha protein degradation incubated for 8 to 22 hrs by immunofluorescence assay	ic50	0.0004	uM
3-[6-[4-[2-[1-[5-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyrimidin-2-yl]piperidin-4-yl]ethyl]piperazin-1-yl]-4-methoxy-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1678557: Protac activity at CRBN/ERalpha in human MCF7 cells assessed as induction of ERalpha protein degradation incubated for 8 to 22 hrs by immunofluorescence assay	ic50	0.0004	uM
3-[6-[4-[[9-[5-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyrimidin-2-yl]oxy-3-azaspiro[5.5]undecan-3-yl]methyl]piperidin-1-yl]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1678557: Protac activity at CRBN/ERalpha in human MCF7 cells assessed as induction of ERalpha protein degradation incubated for 8 to 22 hrs by immunofluorescence assay	ic50	0.0004	uM
5-[4-[[4-[[2-(2,6-dioxopiperidin-3-yl)-1-oxo-3H-isoindol-4-yl]oxymethyl]phenyl]methyl]piperazin-1-yl]pyridine-2-carboxamide	1667517: Induction of CRBN-mediated pLOC-ePL-tagged aiolos (unknown origin) degradation in human DF15 cells assessed as minimum protein remaining incubated for 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay	ec50	0.0004	uM
4-[[4-[1-[3-(cyanomethyl)-1-ethylsulfonylazetidin-3-yl]pyrazol-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-N-[2-[4-[4-(2,6-dioxopiperidin-3-yl)phenyl]piperazin-1-yl]ethyl]benzamide	1827294: Binding affinity to CRBN (unknown origin) measured by Fluorescent Polarization assay	ic50	0.0004	uM
N-[2-[4-[[3-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]propyl-methylamino]methyl]cyclohexyl]-6-(2-hydroxypropan-2-yl)indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide	2085323: Binding affinity to CRBN/IRAK4 in human OCI-Ly10 cells assessed as dissociation constant by DiscoverX Kd Elect assay	kd	0.0004	uM
3-[6-[10-[2-[1-[5-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyrimidin-2-yl]piperidin-4-yl]ethyl]-7-oxa-3,10-diazaspiro[5.6]dodecan-3-yl]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1678557: Protac activity at CRBN/ERalpha in human MCF7 cells assessed as induction of ERalpha protein degradation incubated for 8 to 22 hrs by immunofluorescence assay	ic50	0.0005	uM
3-[6-[4-[2-[1-[5-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyrimidin-2-yl]piperidin-4-yl]ethyl]piperazin-1-yl]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1678557: Protac activity at CRBN/ERalpha in human MCF7 cells assessed as induction of ERalpha protein degradation incubated for 8 to 22 hrs by immunofluorescence assay	ic50	0.0005	uM
3-[6-[4-[2-[1-[5-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyrimidin-2-yl]piperidin-4-yl]oxyethyl]piperazin-1-yl]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1678557: Protac activity at CRBN/ERalpha in human MCF7 cells assessed as induction of ERalpha protein degradation incubated for 8 to 22 hrs by immunofluorescence assay	ic50	0.0005	uM
N-[3-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]propyl]-4-[[4-(1-propylpyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]benzamide	1710172: PROTAC activity at CRBN/JAK2 in human MHHCALL4 cells assessed as protein degradation by immunoblot analysis	ec50	0.0005	uM
4-[[4-[1-[3-(cyanomethyl)-1-ethylsulfonylazetidin-3-yl]pyrazol-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-N-[4-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]butyl]benzamide	1710172: PROTAC activity at CRBN/JAK2 in human MHHCALL4 cells assessed as protein degradation by immunoblot analysis	ec50	0.0005	uM
(3R)-3-[7-[[4-[[4-(2,4-difluorophenyl)piperazin-1-yl]methyl]phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1667517: Induction of CRBN-mediated pLOC-ePL-tagged aiolos (unknown origin) degradation in human DF15 cells assessed as minimum protein remaining incubated for 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay	ec50	0.0005	uM
3-[7-[[4-[[4-(4-methoxyphenyl)piperazin-1-yl]methyl]phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1667517: Induction of CRBN-mediated pLOC-ePL-tagged aiolos (unknown origin) degradation in human DF15 cells assessed as minimum protein remaining incubated for 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay	ec50	0.0005	uM
N-[5-[[2-(2,6-dioxopiperidin-3-yl)-1-oxo-3H-isoindol-4-yl]amino]pentyl]-4-[[4-(1-propylpyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]benzamide	1710172: PROTAC activity at CRBN/JAK2 in human MHHCALL4 cells assessed as protein degradation by immunoblot analysis	ec50	0.0005	uM
6-[2-[2-[6-[4-[3-[3-cyano-4-(2,4-dichloro-5-methoxyanilino)-6-methoxyquinolin-7-yl]oxypropyl]piperazin-1-yl]hexoxy]ethoxy]ethoxy]-N-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]hexanamide	1678549: Protac binding affinity at CRBN/BCR-ABL (unknown origin) assessed as binding to phosphorylated c-ABL kinase domain by Kinomescan assay	kd	0.0006	uM
3-[6-[4-[[4-[[1-[5-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyrimidin-2-yl]piperidin-4-yl]methyl]piperazin-1-yl]methyl]piperidin-1-yl]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1678557: Protac activity at CRBN/ERalpha in human MCF7 cells assessed as induction of ERalpha protein degradation incubated for 8 to 22 hrs by immunofluorescence assay	ic50	0.0006	uM
3-[6-[4-[5-[3,5-difluoro-4-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenoxy]pentyl]piperazin-1-yl]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1678557: Protac activity at CRBN/ERalpha in human MCF7 cells assessed as induction of ERalpha protein degradation incubated for 8 to 22 hrs by immunofluorescence assay	ic50	0.0006	uM
3-[7-[[4-[[4-(2,4-dichlorophenyl)-2-oxopiperazin-1-yl]methyl]phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1667517: Induction of CRBN-mediated pLOC-ePL-tagged aiolos (unknown origin) degradation in human DF15 cells assessed as minimum protein remaining incubated for 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay	ec50	0.0006	uM
4-[4-[[[2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetyl]amino]methyl]piperidin-1-yl]-N-(2,6-dioxopiperidin-3-yl)-2-methoxybenzamide	2021014: Protac activity at BRD4 in human MOLT-4 cells assessed as BRD4 protein degradation incubated for 24 hrs by immunoblotting analysis	ec50	0.0006	uM
3-[6-[4-[[1-[5-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyrimidin-2-yl]piperidin-4-yl]methyl]piperazin-1-yl]-4-methoxy-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1678557: Protac activity at CRBN/ERalpha in human MCF7 cells assessed as induction of ERalpha protein degradation incubated for 8 to 22 hrs by immunofluorescence assay	ic50	0.0007	uM
3-[7-[[4-[[4-(5-fluoro-2-pyridinyl)piperazin-1-yl]methyl]phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione	1667517: Induction of CRBN-mediated pLOC-ePL-tagged aiolos (unknown origin) degradation in human DF15 cells assessed as minimum protein remaining incubated for 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay	ec50	0.0007	uM

CTD chemical–gene interactions

42 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
pomalidomide	increases response to substance, affects binding, affects cotreatment, increases expression, decreases reaction (+2 more)	4
Lenalidomide	increases response to substance, affects binding, decreases reaction, increases degradation, increases ubiquitination	4
Thalidomide	affects response to substance, affects binding, decreases reaction, increases degradation, increases ubiquitination	3
cobaltous chloride	increases expression	2
Air Pollutants	decreases expression, affects expression, increases abundance	2
Valproic Acid	decreases expression, increases expression	2
GSK-J4	increases expression	1
afuresertib	affects cotreatment, increases expression	1
ginger extract	affects cotreatment, affects expression, increases abundance	1
dicrotophos	decreases expression	1
methylmercuric chloride	decreases expression	1
triphenyl phosphate	affects expression	1
bisphenol A	affects cotreatment, affects expression, increases abundance	1
mono-(2-ethylhexyl)phthalate	decreases expression	1
sodium arsenite	increases abundance, increases expression	1
tobacco tar	decreases expression	1
4-aminophenylarsenoxide	affects binding, decreases reaction	1
cylindrospermopsin	increases expression	1
tri-isobutylphosphate	affects expression	1
K 7174	increases expression	1
abrine	increases expression	1
2-(1H-indazol-4-yl)-6-(4-methanesulfonylpiperazin-1-ylmethyl)-4-morpholin-4-ylthieno(3,2-d)pyrimidine	increases expression, increases response to substance	1
jinfukang	decreases expression	1
3-(2-hydroxy-4-(2-methylnonan-2-yl)phenyl)cyclohexan-1-ol	decreases expression	1
Sunitinib	increases expression	1
Arsenic Trioxide	affects binding, decreases reaction	1
Arsenic	increases abundance, increases expression	1
Benzo(a)pyrene	increases methylation	1
Dexamethasone	affects cotreatment, increases expression	1
Formaldehyde	increases expression	1

ChEMBL screening assays

5948 unique, capped per target: 5779 binding, 154 functional, 15 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3768094	Binding	Binding affinity to human CRBN (delta 1 to 315) by FRET assay	A FRET-Based Assay for the Identification and Characterization of Cereblon Ligands. — J Med Chem
CHEMBL5346088	Functional	In vivo protac activity at CRBN/IKZF1 in CB17-SCID mouse xenografted with human TMD8 cells assessed as degradation of IKZF1 protein in tumor at 10 to 90 mg/kg,po administration for 25 days by flow cytomtery	Discovery and Preclinical Pharmacology of NX-2127, an Orally Bioavailable Degrader of Bruton’s Tyrosine Kinase with Immunomodulatory Activity for the Treatment of Patients with B Cell Malignancies. — J Med Chem
CHEMBL4610576	ADMET	Protac activity at cereblon/cullin4A/BRD3 in human MV4-11 cells assessed as induction of BRD3 degradation at 50 nM measured after 18 hrs by Western blot analysis	Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies. — Bioorg Med Chem

Cellosaurus cell lines

12 cell lines: 11 cancer cell line, 1 transformed cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_B8E0	Abcam HCT 116 CRBN KO	Cancer cell line	Male
CVCL_B9G8	Abcam A-549 CRBN KO	Cancer cell line	Male
CVCL_D2EK	Abcam MCF-7 CRBN KO	Cancer cell line	Female
CVCL_D7G8	Ubigene HEK293T CRBN KO	Transformed cell line	Female
CVCL_D7MT	Ubigene A-549 CRBN KO	Cancer cell line	Male
CVCL_E0AT	Ubigene HeLa CRBN KO	Cancer cell line	Female
CVCL_E0TW	Ubigene Hep G2 CRBN KO	Cancer cell line	Male
CVCL_E8T6	MCF7 CRBN KO clone 2A3	Cancer cell line	Female
CVCL_F1UW	HyCyte U-937 KO-hCRBN	Cancer cell line	Male
CVCL_SJ69	HAP1 CRBN (-) 1	Cancer cell line	Male

Clinical trials (associated diseases)

300 trials via MONDO — disease-level, not drug-specific.

Trial	Phase	Status	Title
NCT05657860	PHASE4	COMPLETED	Guanfacine Extended Release for the Reduction of Aggression and Self-injurious Behavior Associated With Prader-Willi Syndrome
NCT05744479	PHASE4	RECRUITING	Metformin for Antipsychotic-induced Weight Gain in Adults With Intellectual Disability
NCT06107829	PHASE4	WITHDRAWN	Valbenazine Treatment of Tardive Dyskinesia in Adults With Intellectual/Developmental Disabilities
NCT06997198	PHASE4	NOT_YET_RECRUITING	Deutetrabenazine Treatment for Tardive Dyskinesia in Intellectual/Developmental Disabilities
NCT00029224	PHASE4	COMPLETED	Treatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions
NCT00104104	PHASE4	COMPLETED	A Multiple Myeloma Trial in Patients With Bone Metastases
NCT00211211	PHASE4	COMPLETED	FREE Study - Fracture Reduction Evaluation
NCT00242528	PHASE4	WITHDRAWN	Open-label Study, to Evaluate the Safety and Tolerability of Zoledronic Acid in Patients With Bone Lesions Secondary to Multiple Myeloma.
NCT00257114	PHASE4	COMPLETED	Evaluation of VELCADE Given as Retreatment to Multiple Myeloma Patients for Efficacy, Safety and Tolerability
NCT00352703	PHASE4	COMPLETED	PROMPT - Palifermin in Reduction of Oral Mucositis in PBSC Transplantation
NCT00361140	PHASE4	COMPLETED	Busulfan Safety/Efficacy as Conditioning Prior to Hematopoietic Cell Transplantation (HCT)
NCT00622505	PHASE4	COMPLETED	Zoledronic Acid Treatment (Every 4 or 12 Weeks) to Prevent Skeletal Complications in Advanced Multiple Myeloma Participants
NCT00652041	PHASE4	COMPLETED	Bortezomib/Adriamycine/Melfalan/Prednisone (VAMP)/Thalidomide/Cyclophosphamide/Dexamethasone (TaCyDex) or Bortezomib/Melfalan/Prednisone (V-MP)/TaCyDex) in Refractary or Relapsed Multiple Myeloma
NCT00733538	PHASE4	COMPLETED	Stage I Multiple Myeloma Treatment
NCT01087008	PHASE4	COMPLETED	Zoledronic Acid in Patients With Multiple Myeloma and Asymptomatic Biochemical Relapse
NCT01249690	PHASE4	UNKNOWN	Efficacy Study of PAD and TAD in Newly Diagnosed Multiple Myeloma
NCT01410929	PHASE4	WITHDRAWN	Evaluation of Vertebral Compression Fracture Fixation With RF Kyphoplasty in Patients With Multiple Myeloma
NCT01731886	PHASE4	COMPLETED	Lenalidomide and Dexamethasone With/Without Stem Cell Transplant in Patients With Multiple Myeloma
NCT01868828	PHASE4	UNKNOWN	A Study of PAD Versus Velcade, Cyclophosphamide and Dexamethasone (VCD) Treatment in Subjects With Multiple Myeloma
NCT02268890	PHASE4	COMPLETED	A Pharmacokinetic Study of Bortezomib in Taiwanese Participants With Multiple Myeloma
NCT02286830	PHASE4	COMPLETED	Prolonged Protection From Bone Disease in Multiple Myeloma
NCT02559154	PHASE4	UNKNOWN	Modified Bortezomib-based Combination Therapy for Multiple Myeloma
NCT02577783	PHASE4	UNKNOWN	PDD vs PAD to Treat Initially Diagnosed MM
NCT02773550	PHASE4	TERMINATED	Treatment With a Scheme With Low Doses of Bortezomib / Melphalan / Prednisone (MPV) in Patients With Multiple Myeloma
NCT02958969	PHASE4	COMPLETED	Apixaban for Primary Prevention of Venous Thromboembolism in Patients With Multiple Myeloma
NCT03173092	PHASE4	TERMINATED	A Study of Ixazomib (NINLARO®) in Combination With Lenalidomide and Dexamethasone (IRD) for the Treatment of Participants With Multiple Myeloma (MM)
NCT03619252	PHASE4	COMPLETED	Pneumococcal Vaccination of Multiple Myeloma Patients on Novel Agents
NCT03768960	PHASE4	COMPLETED	A Study of DARZALEX (Daratumumab) In Indian Participants With Relapsed and Refractory Multiple Myeloma, Whose Prior Therapy Included a Proteasome Inhibitor and an Immunomodulatory Agent
NCT03829371	PHASE4	ACTIVE_NOT_RECRUITING	STUDY COMPARING TWO STANDARD TREATMENTS IN AUTOLOGOUS STEM CELL TRANSPLANTATION INELIGIBLE POPULATION AFFECTED BY MULTIPLE MYELOMA
NCT03908138	PHASE4	UNKNOWN	RDD Versus VDD in Newly Diagnosed Patients With Multiple Myeloma
NCT04217967	PHASE4	COMPLETED	Ixazomib, Lenalidomide, and Combination for Maintenance in NDMM Patients
NCT04952766	PHASE4	COMPLETED	Study Evaluating SARS-CoV-2 (COVID-19) Humoral Response After BNT162b2 Vaccine in Immunocompromised Adults Compared to Healthy Adults
NCT04989140	PHASE4	UNKNOWN	Study of Pomalidomide, Oral Dexamethasone and Ixazomib in Patients With Relapsed MM Who Have Received Lenalidomide
NCT05183139	PHASE4	WITHDRAWN	A Multicenter In-class Transition Study of Ixazomib Combined With Pomalidomide and Dexamethasone or With Lenalidomide and Dexamethasone in Adults With Relapsed/Refractory Multiple Myeloma
NCT05201781	PHASE4	RECRUITING	A Long-term Study for Participants Previously Treated With Ciltacabtagene Autoleucel
NCT05429515	PHASE4	NOT_YET_RECRUITING	Effect of HFR-SUPRA in the Treatment of Multiple Myeloma-related Acute Kidney Injury
NCT05511428	PHASE4	COMPLETED	Home Based Daratumumab Administration for Patients With Multiple Myeloma
NCT05545202	PHASE4	UNKNOWN	A Randomized, Comparative, Double-blind Trial of Pentaisomaltose and Dimethyl Sulphoxide for Cryoprotection of Hematopoietic Stem Cells in Subjects With Multiple Myeloma or Malignant Lymphoma With a Need for Autologous Transplantation
NCT05555329	PHASE4	COMPLETED	Alternative Dosing Scheme of Pomalidomide 4 mg Every Other Day Versus Pomalidomide 2 mg and 4 mg Every Day; the POMAlternative Study
NCT05722405	PHASE4	RECRUITING	Ixazomib Plus Low-dose Lenalidomide Versus Ixazomib Alone for Maintenance Treatment of High Risk Multiple Myeloma