BCL6

Summary

BCL6 (BCL6 transcription repressor, HGNC:1001) is a protein-coding gene on chromosome 3q27.3, encoding B-cell lymphoma 6 protein (P41182). Transcriptional repressor mainly required for germinal center (GC) formation and antibody affinity maturation which has different mechanisms of action specific to the lineage and biological functions.

The protein encoded by this gene is a zinc finger transcription factor and contains an N-terminal POZ domain. This protein acts as a sequence-specific repressor of transcription, and has been shown to modulate the transcription of STAT-dependent IL-4 responses of B cells. This protein can interact with a variety of POZ-containing proteins that function as transcription corepressors. This gene is found to be frequently translocated and hypermutated in diffuse large-cell lymphoma (DLCL), and may be involved in the pathogenesis of DLCL. Alternatively spliced transcript variants encoding different protein isoforms have been found for this gene.

Source: NCBI Gene 604 — RefSeq curated summary.

At a glance

• GWAS associations: 26
• Clinical variants (ClinVar): 96 total — 1 pathogenic
• Phenotypes (HPO): 17
• Druggable target: yes — 2 molecules with ChEMBL bioactivity
• Cancer driver (intOGen): activating (oncogene-like) across 2 cancer types
• Transcription factor: yes — 109 downstream targets (CollecTRI)
• MANE Select transcript: NM_001706

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:1001
Approved symbol	BCL6
Name	BCL6 transcription repressor
Location	3q27.3
Locus type	gene with protein product
Status	Approved
Aliases	ZBTB27, LAZ3, BCL5, BCL6A
Ensembl gene	ENSG00000113916
Ensembl biotype	protein_coding
OMIM	109565
Entrez	604

Gene structure

Transcript identifiers

Ensembl transcripts: 11 — 6 protein_coding, 2 retained_intron, 2 protein_coding_CDS_not_defined, 1 nonsense_mediated_decay

ENST00000232014, ENST00000406870, ENST00000419510, ENST00000430339, ENST00000438077, ENST00000450123, ENST00000470319, ENST00000479110, ENST00000480458, ENST00000496823, ENST00000621333

RefSeq mRNA: 3 — MANE Select: NM_001706 NM_001130845, NM_001134738, NM_001706

CCDS: CCDS3289, CCDS46975

Canonical transcript exons

ENST00000406870 — 10 exons

Exon	Start	End
ENSE00000781579	187731709	187731930
ENSE00001377234	187734869	187734907
ENSE00001564372	187745410	187745468
ENSE00003458337	187733533	187733703
ENSE00003468191	187724941	187725078
ENSE00003532311	187728360	187728544
ENSE00003540935	187725499	187725629
ENSE00003602776	187729050	187730021
ENSE00003627638	187726731	187726898
ENSE00003841213	187721381	187722601

Expression profiles

Bgee: expression breadth ubiquitous, 300 present calls, max score 99.29.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 41.4260 / max 2570.4251, expressed in 1792 samples.

FANTOM5 promoters (10 alternative TSS)

Promoter ID	TPM avg	Samples expressed
46015	23.9998	1730
46013	8.7266	1225
46012	4.5396	549
46014	2.7790	1054
46005	0.3902	145
46007	0.3543	158
46004	0.2558	99
46006	0.1698	68
46008	0.1132	54
46003	0.0978	37

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
gastrocnemius	UBERON:0001388	99.29	gold quality
mucosa of stomach	UBERON:0001199	99.11	gold quality
blood	UBERON:0000178	99.08	gold quality
left uterine tube	UBERON:0001303	99.06	gold quality
muscle of leg	UBERON:0001383	99.06	gold quality
pericardium	UBERON:0002407	98.89	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	98.89	gold quality
right lung	UBERON:0002167	98.85	gold quality
upper leg skin	UBERON:0004262	98.79	gold quality
gluteal muscle	UBERON:0002000	98.78	gold quality
bronchial epithelial cell	CL:0002328	98.69	gold quality
skin of abdomen	UBERON:0001416	98.69	gold quality
muscle organ	UBERON:0001630	98.68	gold quality
skeletal muscle organ	UBERON:0014892	98.68	gold quality
skin of leg	UBERON:0001511	98.66	gold quality
nerve	UBERON:0001021	98.60	gold quality
tibial nerve	UBERON:0001323	98.60	gold quality
deltoid	UBERON:0001476	98.59	gold quality
cartilage tissue	UBERON:0002418	98.58	gold quality
subcutaneous adipose tissue	UBERON:0002190	98.50	gold quality
vena cava	UBERON:0004087	98.48	gold quality
tibialis anterior	UBERON:0001385	98.47	gold quality
peritoneum	UBERON:0002358	98.47	gold quality
omental fat pad	UBERON:0010414	98.47	gold quality
adipose tissue of abdominal region	UBERON:0007808	98.46	gold quality
zone of skin	UBERON:0000014	98.41	gold quality
popliteal artery	UBERON:0002250	98.39	gold quality
tibial artery	UBERON:0007610	98.39	gold quality
skin of hip	UBERON:0001554	98.37	gold quality
hindlimb stylopod muscle	UBERON:0004252	98.34	gold quality

Single-cell (SCXA)

Detected in 4 experiment(s), a significant marker in 4.

Experiment	Marker?	Max mean expression
E-GEOD-180759	yes	2004.10
E-MTAB-9067	yes	12.50
E-MTAB-6678	yes	8.01
E-ANND-3	no	0.00

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

109 targets.

Target	Regulation
ABL1
ADAM2
AKT1
AP1
ARID1B
ATR	Repression
BCL2
BCL2L1	Repression
BCL6	Repression
BCR
BMI1
CASP1
CCL1	Activation
CCL11	Activation
CCL13	Activation
CCL17	Activation
CCL2	Activation
CCL3	Repression
CCL4	Repression
CCL7	Activation
CCL8	Repression
CCNA2	Repression
CCND1	Activation
CCND2	Repression
CCR7
CD22
CD63
CD79A
CD80	Repression
CD8A

JASPAR motifs

Motif	Name	Family
MA0463.2	BCL6	More than 3 adjacent zinc fingers
MA0463.3	BCL6	More than 3 adjacent zinc fingers

JASPAR matrix evidence (PMIDs): PMID:7945383

Upstream regulators (CollecTRI, top): ABL1, BCL6, CTCF, FOSL2, FOXO3, FOXO4, GLI2, IL21, IRF4, IRF8, JUND, MEF2B, MYC, NANOG, PATZ1, PRDM1, SPI1, STAT1, STAT3, STAT5A, STAT5B, STAT6, TP53, ZEB1

miRNA regulators (miRDB)

164 targeting BCL6, 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-190A-3P	100.00	80.35	5520
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-LET-7A-3P	100.00	74.03	3932
HSA-LET-7B-3P	100.00	74.08	3913
HSA-LET-7F-1-3P	100.00	74.02	3928
HSA-MIR-98-3P	100.00	74.08	3907
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-30A-5P	100.00	76.31	3233
HSA-MIR-30B-5P	100.00	76.29	3248
HSA-MIR-30C-5P	100.00	76.29	3248
HSA-MIR-30D-5P	100.00	76.32	3233
HSA-MIR-30E-5P	100.00	76.32	3242
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-188-3P	100.00	68.76	1240
HSA-MIR-8485	100.00	77.57	4731
HSA-MIR-9-5P	100.00	72.28	2361
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-4789-3P	99.99	70.75	2484
HSA-MIR-548AW	99.99	72.57	3559
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-34A-5P	99.99	71.21	1784
HSA-MIR-449A	99.99	71.05	1776
HSA-MIR-3185	99.99	68.12	1959
HSA-LET-7F-2-3P	99.98	70.98	2588
HSA-MIR-1185-1-3P	99.98	71.04	2593
HSA-MIR-1185-2-3P	99.98	71.04	2593
HSA-MIR-548AN	99.97	70.91	2817
HSA-MIR-34C-5P	99.97	70.45	1577
HSA-MIR-449B-5P	99.97	70.26	1580

Literature-anchored findings (GeneRIF, showing 40)

• BCL6 may regulate apoptosis by means of its repressive effects on PDCD2 (PMID:11854457)
• A senescence rescue screen identifies BCL6 as an inhibitor of anti-proliferative p19(ARF)-p53 signaling (PMID:11914273)
• gene reearranged in non-hodkgin’s lymphoma (PMID:11920179)
• Class II histone deacetylases are directly recruited by BCL6 transcriptional repressor (PMID:11929873)
• Bcl6 mediates repression of IL-5 gene expression by binding specifically to a DNA sequence on the 3’ untranslated region of the IL-5 gene. (PMID:12097386)
• BCL-6 regulates the Blimp-1 promoter through a novel mechanism involving AP-1 elements. (PMID:12165517)
• bcl-2/Jh lymphomas show molecular heterogeneity and that bcl-6 and p53 mutations may be acquired during the evolution of such lymphomas (PMID:12217802)
• REVIEW: those BCL6 translocations with non-immunoglobulin genes placing the rearranged BCL6 gene under the control of the replaced promoter activity; its role in pathogenesis of diffuse large b-cell lymphomas (PMID:12389616)
• Frequent occurrence of BCL6 rearrangements in nodular lymphocyte predominance Hodgkin lymphoma but not in classical Hodgkin lymphoma indicate a significant role of BCL6 in the pathogenesis of NLPHL. (PMID:12393409)
• Role of BCL6 in B cell development and in lymphoma [review] (PMID:12469325)
• the distinct profile of BCL-6 expression in Jijoye/Clone-13 is due to either a missing negative element in a different portion of the gene or that there is an issue of chromatin accessibility operating in BCL-6 gene regulation (PMID:12477975)
• high frequency of BCL-6 mutations discovered in primary mediastinal B-cell lymphoma (PMID:12507907)
• A subset of mutations specifically associated with diffuse large B-cell lymphoma pathogenesis causes deregulated BCL6 transcription by preventing BCL6 from binding its own promoter, thereby disrupting its negative autoregulatory circuit. (PMID:12515714)
• plays a role in immune memory development–review (PMID:12518453)
• role in cell survival and transformation (PMID:12555064)
• Expression of Bcl-6 in primary central nervous system diffuse large B-cell lymphoma may be a prognostic marker for poor overall survival. (PMID:12562237)
• Junctional sequences indicate translocation origins from earlier BCL-6 mutations and switch recombinase events in non-Hodgkin B-cell lymphoma (PMID:12775568)
• tumor specimens expressed BCL6 mRNA predominantly from the rearranged allele that may come under the control of various partner gene promoters (PMID:12835729)
• results show that BCL6 prevents CD40-induced expression of CD80 by binding its promoter region in vivo and suppressing its transcriptional activation by NF-kappaB (PMID:12860928)
• bcl-2 and bcl-6 proteins may play a role in the pathogenesis of transitional cell carcinoma, and bcl-6 expression reflects histopathologic grade. (PMID:12879322)
• BCL6 overexpression was found to inhibit the increase in ROS levels and apoptosis in response to etoposide and other chemotherapeutic reagents. (PMID:12881702)
• BCL-6 oncogene activation plays a role in breast cancers, not just lymphomas. (PMID:14654791)
• This study suggest translocation-mediated BCL6 oncogene activation as a so far unknown pathogenetically relevant mechanism in PCNSL. (PMID:14655758)
• Data describe a 17 residue fragment from SMRT that binds to the BCL6 BTB domain, and report the crystal structure of the complex to 2.2 angstroms. (PMID:14690607)
• BCL6 translocation has a pathogenic in B-cell non-Hodgkin’s lymphoma (review) (PMID:15024721)
• Rearrangements of the BCL6 locus were detected in five B-cell lymphomas of the leg, and involved IGH (two cases), IGL (one case), and non-IG genes (two cases). (PMID:15191563)
• REVIEW recently identified deacetylation pathways resulting in the accumulation of inactive acetylated Bcl-6 and thus in cell cycle arrest and apoptosis in B-cell lymphoma cell (PMID:15202519)
• Cytogenetic alterations affecting BCL6 are predominantly found in follicular lymphomas grade 3B with a diffuse large B-cell component (PMID:15277222)
• Nodular lymphocyte-predominant Hodgkin’s lymphoma (NLPHL) showed recurrent rearrangement of the BCL6 gene. (PMID:15339680)
• Meta-analysis showed that the preferentially altered sequence motifs of BCL6 in PMBL were TA & AT and TAT. GC & RGYW/WRCY motifs were a target in DLCL & FL but not in PMBL. Nucleotides 150-270 were highly targeted only in PMBL. (PMID:15377470)
• conditional activation of FoxO3a leads to accumulation of BCL6 and down-regulation of cyclin D2 at protein and mRNA levels (PMID:15509806)
• an important function of BCL6 is possibly to allow germinal-centre B cells to tolerate the physiological DNA breaks required for immunoglobulin class switch recombination and somatic hypermutation without inducing a p53-dependent apoptotic response (PMID:15577913)
• Point mutations in the 5’ noncoding region of BCL-6 gene are found in Chinese patients with primary gastric lymphomas and MALT lymphomas (PMID:15609396)
• single-nucleotide polymorphisms and acquired somatic mutations of the BCL6 first intron is associated with follicular lymphoma (PMID:16094416)
• Many of the novel binsubf proteins identified in this study suggest additional functional roles for BCL6 beyond transcriptional repression. (PMID:16147992)
• We present here a case of Follicular Lymphoma with leukemic presentation and a complex translocation involving the IgH, BCL2 and BCL6 loci (PMID:16194898)
• BCL6 gene is a new p53 target, regulated through a p53 response element in B-cell lymphoma. (PMID:16249378)
• Our results support the hypothesis that a genetic variant that could alter mRNA transcripts of BCL6 may contribute to the etiology of NHL (non-Hodgkin lymphoma). (PMID:16264183)
• By regulating the induction of several genes implicated in the immune response, including inflammatory cytokines, chemokines and survival genes, BCL6 may represent a pivotal modulator of the afferent branch of the immune response. (PMID:16455075)
• BCL-6 expression was asfavorable prognostic factor in patients with diffuse large B-cell lymphoma of central nervous system origin and peripheral nodal origin. (PMID:16489068)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	bcl6ab	ENSDARG00000069295
danio_rerio	bcl6aa	ENSDARG00000070864
mus_musculus	Bcl6	ENSMUSG00000022508
rattus_norvegicus	Bcl6	ENSRNOG00000001843

Paralogs (28): ZNF280C (ENSG00000056277), ZBTB25 (ENSG00000089775), PRDM13 (ENSG00000112238), FEZF1 (ENSG00000128610), ZBTB46 (ENSG00000130584), PRDM12 (ENSG00000130711), ZNF280D (ENSG00000137871), NACC2 (ENSG00000148411), FEZF2 (ENSG00000153266), ZBTB7B (ENSG00000160685), NACC1 (ENSG00000160877), BCL6B (ENSG00000161940), GFI1 (ENSG00000162676), GFI1B (ENSG00000165702), ZBTB49 (ENSG00000168826), ZNF280A (ENSG00000169548), ZNF581 (ENSG00000171425), ZNF524 (ENSG00000171443), ZBTB26 (ENSG00000171448), ZBTB21 (ENSG00000173276), ZNF683 (ENSG00000176083), ZBTB33 (ENSG00000177485), ZBTB3 (ENSG00000185670), ZBTB6 (ENSG00000186130), ZBTB14 (ENSG00000198081), ZBTB12 (ENSG00000204366), ZNF580 (ENSG00000213015), ZNF280B (ENSG00000275004)

Protein

Protein identifiers

B-cell lymphoma 6 protein — P41182 (reviewed: P41182)

Alternative names: B-cell lymphoma 5 protein, Protein LAZ-3, Zinc finger and BTB domain-containing protein 27, Zinc finger protein 51

All UniProt accessions (4): P41182, A0A0C4DH53, C9JCS5, C9JL16

UniProt curated annotations — full annotation on UniProt →

Function. Transcriptional repressor mainly required for germinal center (GC) formation and antibody affinity maturation which has different mechanisms of action specific to the lineage and biological functions. Forms complexes with different corepressors and histone deacetylases to repress the transcriptional expression of different subsets of target genes. Represses its target genes by binding directly to the DNA sequence 5’-TTCCTAGAA-3’ (BCL6-binding site) or indirectly by repressing the transcriptional activity of transcription factors. In GC B-cells, represses genes that function in differentiation, inflammation, apoptosis and cell cycle control, also autoregulates its transcriptional expression and up-regulates, indirectly, the expression of some genes important for GC reactions, such as AICDA, through the repression of microRNAs expression, like miR155. An important function is to allow GC B-cells to proliferate very rapidly in response to T-cell dependent antigens and tolerate the physiological DNA breaks required for immunoglobulin class switch recombination and somatic hypermutation without inducing a p53/TP53-dependent apoptotic response. In follicular helper CD4(+) T-cells (T(FH) cells), promotes the expression of T(FH)-related genes but inhibits the differentiation of T(H)1, T(H)2 and T(H)17 cells. Also required for the establishment and maintenance of immunological memory for both T- and B-cells. Suppresses macrophage proliferation through competition with STAT5 for STAT-binding motifs binding on certain target genes, such as CCL2 and CCND2. In response to genotoxic stress, controls cell cycle arrest in GC B-cells in both p53/TP53-dependedent and -independent manners. Besides, also controls neurogenesis through the alteration of the composition of NOTCH-dependent transcriptional complexes at selective NOTCH targets, such as HES5, including the recruitment of the deacetylase SIRT1 and resulting in an epigenetic silencing leading to neuronal differentiation.

Subunit / interactions. Homodimer. Interacts (via BTB domain) with the corepressors BCOR, NCOR1 and SMRT/NCOR2; the interactions are direct. Forms preferably ternary complexes with BCOR and SMRT/NCOR2 on target gene promoters but, on enhancer elements, interacts with SMRT/NCOR2 and HDAC3 to repress proximal gene expression. Interacts with histone deacetylases HDAC2, HDAC5 and HDAC9 (via the catalytic domain). Interacts with ZBTB7 and BCL6B. Interacts with SCF(FBXO11) complex; the interaction is independent of phosphorylation and promotes ubiquitination. Interacts (when phosphorylated) with PIN1; the interaction is required for BCL6 degradation upon genotoxic stress. Interacts with ZBTB17; inhibits ZBTB17 transcriptional activity. Interacts with CTBP1, autoinhibits its transcriptional expression. Interacts with NOTCH1 NCID and SIRT1; leads to a epigenetic repression of selective NOTCH1-target genes. Interacts (nor via BTB domain neither acetylated) with the NuRD complex components CHD4, HDAC1, MBD3 and MTA3; the interaction with MTA3 inhibits BCL6 acetylation and is required for BCL6 transpriptional repression.

Subcellular location. Nucleus.

Tissue specificity. Expressed in germinal center T- and B-cells and in primary immature dendritic cells.

Post-translational modifications. Phosphorylated by MAPK1 in response to antigen receptor activation at Ser-333 and Ser-343. Phosphorylated by ATM in response to genotoxic stress. Phosphorylation induces its degradation by ubiquitin/proteasome pathway. Polyubiquitinated. Polyubiquitinated by SCF(FBXO11), leading to its degradation by the proteasome. Ubiquitinated by the SCF(FBXL17) complex, leading to its degradation by the proteasome: ubiquitination by the SCF(FBXL17) complex takes place when aberrant BTB domain dimers are formed. Acetylated at Lys-379 by EP300 which inhibits the interaction with NuRD complex and the transcriptional repressor function. Deacetylated by HDAC- and SIR2-dependent pathways.

Disease relevance. Chromosomal aberrations involving BCL6 are a cause of B-cell non-Hodgkin lymphomas (B-cell NHL), including diffuse large B-cell lymphoma and follicular lymphoma. Approximately 40% of diffuse large B-cell lymphomas and 5 to 10% of follicular lymphomas are associated with chromosomal translocations that deregulate expression of BCL6 by juxtaposing heterologous promoters to the BCL6 coding domain. Translocation t(3;14)(q27;q32). Translocation t(3;22)(q27;q11) with immunoglobulin gene regions. Translocation t(3;7)(q27;p12) with IKZF1 gene 5’non-coding region. Translocation t(3;6)(q27;p21) with Histone H4. Translocation t(3;16)(q27;p11) with IL21R. Translocation t(3;13)(q27;q14) with LCP1. A chromosomal aberration involving BCL6 may be a cause of a form of B-cell leukemia. Translocation t(3;11)(q27;q23) with POU2AF1/OBF1. A chromosomal aberration involving BCL6 may be a cause of lymphoma. Translocation t(3;4)(q27;p11) with ARHH/TTF.

Domain organisation. The BTB domain mediates homodimerization. Its dimer interface mediates peptide binding such as to corepressors BCOR and NCOR2. Interaction with corepressors through the BTB domain is needed to facilitate the rapid proliferation and survival of GC B-cells but is not involved in the T(FH) formation and BCL6-mediated suppression of T(H)2 and T(H)17 differentiationrequired for GC formation.

Induction. Down-regulated during maturation of dendritic cells by selective stimuli such as bacterial lipopolysaccharides (LPS), CD40LG and zymosan. Protein levels decreases upon genotoxic stress in a dose- and time-dependent way.

Isoforms (2)

UniProt ID	Names	Canonical?
P41182-1	1	yes
P41182-2	2

RefSeq proteins (3): NP_001124317, NP_001128210, NP_001697* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000210	BTB/POZ_dom	Domain
IPR011333	SKP1/BTB/POZ_sf	Homologous_superfamily
IPR013087	Znf_C2H2_type	Domain
IPR036236	Znf_C2H2_sf	Homologous_superfamily

Pfam: PF00096, PF00651

UniProt features (76 total): mutagenesis site 18, helix 13, strand 13, zinc finger region 6, turn 6, modified residue 5, region of interest 3, compositionally biased region 3, sequence variant 3, sequence conflict 3, chain 1, domain 1, splice variant 1

Structure

Experimental structures (PDB)

246 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
7LWE	X-RAY DIFFRACTION	1.17
7RV1	X-RAY DIFFRACTION	1.17
7OKL	X-RAY DIFFRACTION	1.2
7LWF	X-RAY DIFFRACTION	1.22
7RV4	X-RAY DIFFRACTION	1.25
7RV8	X-RAY DIFFRACTION	1.25
7RUY	X-RAY DIFFRACTION	1.27
7RV2	X-RAY DIFFRACTION	1.29
1R29	X-RAY DIFFRACTION	1.3
7LWG	X-RAY DIFFRACTION	1.3
7RUW	X-RAY DIFFRACTION	1.3
7RUX	X-RAY DIFFRACTION	1.3
7OKG	X-RAY DIFFRACTION	1.32
7LZR	X-RAY DIFFRACTION	1.34
7RV3	X-RAY DIFFRACTION	1.35
5N20	X-RAY DIFFRACTION	1.38
7ZWX	X-RAY DIFFRACTION	1.38
6EW6	X-RAY DIFFRACTION	1.39
6XZZ	X-RAY DIFFRACTION	1.39
7ZWO	X-RAY DIFFRACTION	1.39
7ZWZ	X-RAY DIFFRACTION	1.4
6TOK	X-RAY DIFFRACTION	1.43
7OKJ	X-RAY DIFFRACTION	1.43
6XYX	X-RAY DIFFRACTION	1.44
7Q7S	X-RAY DIFFRACTION	1.44
7RV0	X-RAY DIFFRACTION	1.45
7Q7T	X-RAY DIFFRACTION	1.46
6C3L	X-RAY DIFFRACTION	1.46
7ZWR	X-RAY DIFFRACTION	1.47
7OKE	X-RAY DIFFRACTION	1.48

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P41182-F1	52.89	0.01

Functional residue map

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

Post-translational modifications (5): 333, 343, 361, 379, 404

Mutagenesis-validated functional residues (18):

Position	Phenotype
21	abolishes interaction with ncor2 and hdac2, no effect on interaction with ctbp1 and transcriptional autoinhibition; when
59	abolished ubiquitination by the scf(fbxl17) complex.
116	abolishes interaction with ncor2 and hdac2, no effect on interaction with ctbp1 and transcriptional autoinhibition; when
190	no effect on interaction with pin1.
250	no effect on interaction with pin1.
260	strongly reduces interaction with pin1.
333	decrease in phosphorylation by mapk1.
343	decrease in phosphorylation by mapk1.
376–379	abolishes interaction with hdac2 and mta3 as well as transcriptional repressor and transforming activities. abolishes in
376	no effect on acetylation.
377	no effect on acetylation.
379	abolishes acetylation. no effect on interaction with mta3, ncor1 and ncor2.
520–523	no effect on dna-binding, nuclear localization, transcriptional repression activity and interaction with hdac5.
548–551	no effect on dna-binding, nuclear localization, transcriptional repression activity and interaction with hdac5.
576–579	abolishes dna-binding and transcriptional repression activity, no effect on nuclear localization and interaction with hd
604–607	abolishes dna-binding and transcriptional repression activity, perturbs nuclear localization. no effect on interaction w
632–635	abolishes dna-binding and transcriptional repression activity, no effect on nuclear localization and interaction with hd
660–663	abolishes dna-binding and transcriptional repression activity, perturbs nuclear localization. no effect on interaction w

Function

Pathways and Gene Ontology

Reactome pathways

12 pathways

ID	Pathway
R-HSA-6785807	Interleukin-4 and Interleukin-13 signaling
R-HSA-6803205	TP53 regulates transcription of several additional cell death genes whose specific roles in p53-dependent apoptosis remain uncertain
R-HSA-9614657	FOXO-mediated transcription of cell death genes
R-HSA-1280215	Cytokine Signaling in Immune system
R-HSA-168256	Immune System
R-HSA-212436	Generic Transcription Pathway
R-HSA-3700989	Transcriptional Regulation by TP53
R-HSA-449147	Signaling by Interleukins
R-HSA-5633008	TP53 Regulates Transcription of Cell Death Genes
R-HSA-73857	RNA Polymerase II Transcription
R-HSA-74160	Gene expression (Transcription)
R-HSA-9614085	FOXO-mediated transcription

MSigDB gene sets: 0 (showing top):

GO Biological Process (59): negative regulation of transcription by RNA polymerase II (GO:0000122), cell morphogenesis (GO:0000902), regulation of cytokine production (GO:0001817), negative regulation of cell-matrix adhesion (GO:0001953), plasma cell differentiation (GO:0002317), germinal center formation (GO:0002467), regulation of germinal center formation (GO:0002634), regulation of immune system process (GO:0002682), negative regulation of B cell apoptotic process (GO:0002903), transcription by RNA polymerase II (GO:0006366), inflammatory response (GO:0006954), DNA damage response (GO:0006974), cell-matrix adhesion (GO:0007160), Rho protein signal transduction (GO:0007266), spermatogenesis (GO:0007283), intracellular protein localization (GO:0008104), pyramidal neuron differentiation (GO:0021859), actin cytoskeleton organization (GO:0030036), negative regulation of cell growth (GO:0030308), positive regulation of B cell proliferation (GO:0030890), heterochromatin formation (GO:0031507), negative regulation of mast cell cytokine production (GO:0032764), negative regulation of mononuclear cell proliferation (GO:0032945), negative regulation of Rho protein signal transduction (GO:0035024), type 2 immune response (GO:0042092), B cell proliferation (GO:0042100), regulation of cell population proliferation (GO:0042127), regulation of T cell proliferation (GO:0042129), positive regulation of apoptotic process (GO:0043065), regulation of memory T cell differentiation (GO:0043380), T-helper 2 cell differentiation (GO:0045064), positive regulation of regulatory T cell differentiation (GO:0045591), regulation of cell differentiation (GO:0045595), negative regulation of T-helper 2 cell differentiation (GO:0045629), positive regulation of neuron differentiation (GO:0045666), negative regulation of Notch signaling pathway (GO:0045746), negative regulation of DNA-templated transcription (GO:0045892), isotype switching to IgE isotypes (GO:0048289), negative regulation of isotype switching to IgE isotypes (GO:0048294), erythrocyte development (GO:0048821)

GO Molecular Function (16): RNA polymerase II cis-regulatory region sequence-specific DNA binding (GO:0000978), intronic transcription regulatory region sequence-specific DNA binding (GO:0001161), transcription corepressor binding (GO:0001222), DNA-binding transcription repressor activity, RNA polymerase II-specific (GO:0001227), chromatin binding (GO:0003682), DNA-binding transcription factor activity (GO:0003700), zinc ion binding (GO:0008270), chromatin DNA binding (GO:0031490), identical protein binding (GO:0042802), sequence-specific DNA binding (GO:0043565), DNA-binding transcription factor binding (GO:0140297), sequence-specific double-stranded DNA binding (GO:1990837), RNA polymerase II transcription regulatory region sequence-specific DNA binding (GO:0000977), DNA binding (GO:0003677), protein binding (GO:0005515), metal ion binding (GO:0046872)

GO Cellular Component (6): nucleus (GO:0005634), nucleoplasm (GO:0005654), nucleolus (GO:0005730), Golgi apparatus (GO:0005794), paraspeckles (GO:0042382), replication fork (GO:0005657)

Reactome top-level categories

Rollup of top-9 pathways:

Category	Pathways
Generic Transcription Pathway	2
Signaling by Interleukins	1
TP53 Regulates Transcription of Cell Death Genes	1
FOXO-mediated transcription	1
Immune System	1
RNA Polymerase II Transcription	1
Cytokine Signaling in Immune system	1
Transcriptional Regulation by TP53	1
Gene expression (Transcription)	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
transcription cis-regulatory region binding	3
RNA polymerase II transcription regulatory region sequence-specific DNA binding	2
binding	2
DNA binding	2
intracellular membrane-bounded organelle	2
nuclear lumen	2
cellular anatomical structure	2
regulation of transcription by RNA polymerase II	1
transcription by RNA polymerase II	1
negative regulation of DNA-templated transcription	1
anatomical structure morphogenesis	1
cytokine production	1
regulation of gene expression	1
regulation of multicellular organismal process	1
regulation of cell-matrix adhesion	1
cell-matrix adhesion	1
negative regulation of cell-substrate adhesion	1
mature B cell differentiation involved in immune response	1
adaptive immune response based on somatic recombination of immune receptors built from immunoglobulin superfamily domains	1
anatomical structure formation involved in morphogenesis	1
germinal center formation	1
regulation of adaptive immune response based on somatic recombination of immune receptors built from immunoglobulin superfamily domains	1
regulation of anatomical structure morphogenesis	1
immune system process	1
regulation of biological process	1
B cell apoptotic process	1
regulation of B cell apoptotic process	1
negative regulation of lymphocyte apoptotic process	1
DNA-templated transcription	1
defense response	1
cellular response to stress	1
cell-substrate adhesion	1
small GTPase-mediated signal transduction	1
developmental process involved in reproduction	1
male gamete generation	1
macromolecule localization	1
central nervous system neuron differentiation	1
cytoskeleton organization	1
actin filament-based process	1
regulation of cell growth	1

Protein interactions and networks

STRING

3440 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
BCL6	NCOR2	Q9Y618	991
BCL6	NCOR1	O75376	980
BCL6	BCOR	Q6W2J9	979
BCL6	PAX5	Q02548	931
BCL6	HDAC4	P56524	925
BCL6	MME	P08473	921
BCL6	IGHV4-38-2	P0DP08	913
BCL6	TBX21	Q9UL17	909
BCL6	BCL2	P10415	906
BCL6	AICDA	Q9GZX7	898
BCL6	CXCR5	P32302	894
BCL6	IRF4	Q15306	881
BCL6	MYC	P01106	875
BCL6	CD79A	P11912	874
BCL6	CD5	P06127	863

IntAct

188 interactions, top by confidence:

A	B	Type	Score
LIMS4	BCL6	psi-mi:“MI:0915”(physical association)	0.720
BCL6	LIMS4	psi-mi:“MI:0915”(physical association)	0.720
BCL6	TRAF1	psi-mi:“MI:0915”(physical association)	0.700
TRAF1	BCL6	psi-mi:“MI:0915”(physical association)	0.700
BCL6	GOLGA2	psi-mi:“MI:0915”(physical association)	0.700
GOLGA2	BCL6	psi-mi:“MI:0915”(physical association)	0.700
BCL6	BLZF1	psi-mi:“MI:0915”(physical association)	0.680
BLZF1	BCL6	psi-mi:“MI:0915”(physical association)	0.680
BCL6	BCL6	psi-mi:“MI:0915”(physical association)	0.670
BCL6	TRIB3	psi-mi:“MI:0915”(physical association)	0.670
BCL6	FBXO11	psi-mi:“MI:0407”(direct interaction)	0.650
BCL6	FBXO11	psi-mi:“MI:0915”(physical association)	0.650
FBXO11	BCL6	psi-mi:“MI:0914”(association)	0.650
BCL6B	BCL6	psi-mi:“MI:0915”(physical association)	0.560
BCL6	ZBTB7B	psi-mi:“MI:0915”(physical association)	0.560
TLE5	BCL6	psi-mi:“MI:0915”(physical association)	0.560

BioGRID (356): BCL6 (Reconstituted Complex), BCL6 (Affinity Capture-Western), BCL6 (Biochemical Activity), BCL6 (Two-hybrid), BCL6 (Two-hybrid), KIFC3 (Two-hybrid), SIAH1 (Two-hybrid), TRAF1 (Two-hybrid), BLZF1 (Two-hybrid), ZBTB7B (Two-hybrid), CUTC (Two-hybrid), LIMS3 (Two-hybrid), BCL6B (Two-hybrid), BCL6 (Reconstituted Complex), BCL6 (Reconstituted Complex)

ESM2 similar proteins: A0A1D5NS60, A0JN76, A1L2U9, B1WAZ8, E9Q3T6, O15060, O15062, O35260, O93567, P41182, P41183, Q05516, Q0IH98, Q0IJ29, Q0P4X6, Q0V8G8, Q1L8W0, Q3B725, Q3B7N9, Q3SWU4, Q5EAC5, Q5EXX3, Q5R5N5, Q5SW75, Q5ZM39, Q6DDV0, Q6NRK3, Q6NRM8, Q6ZSB9, Q7TQG0, Q7TS63, Q7TSZ8, Q7ZWZ4, Q801P1, Q80X44, Q86VK4, Q8BKX7, Q8BXX2, Q8CII0, Q8NAP3

Diamond homologs: A0A1B8YAB1, A1YPR0, B0WWP2, B1H285, B3M9V8, B3NDN0, B4GRJ2, B4HIK1, B4J045, B4L0G9, B4LIG6, B4MXW3, B4PD06, B4QLQ2, C9JR72, D3Z8N4, E0CZ16, G3X9X1, O15062, O88939, O93567, O95365, P28575, P41182, P41183, Q08CL3, Q08DK3, Q13105, Q16RL8, Q2M0J9, Q3UQV5, Q52KB5, Q5EXX3, Q5R7B8, Q5RDY3, Q5TC79, Q5ZI33, Q5ZKD9, Q5ZM39, Q60821

SIGNOR signaling

18 interactions.

A	Effect	B	Mechanism
FBXO11	down-regulates	BCL6	binding
IL21	“up-regulates quantity by expression”	BCL6	“transcriptional regulation”
BCOR	“up-regulates activity”	BCL6	binding
NCOR1	“up-regulates activity”	BCL6	binding
NCOR2	“up-regulates activity”	BCL6	binding
BCL6	“down-regulates quantity by repression”	LITAF	“transcriptional regulation”
CTCF	“down-regulates quantity by repression”	BCL6	“transcriptional regulation”
BCL6	“down-regulates quantity by repression”	FCER2	“transcriptional regulation”
BCL6	“down-regulates quantity by repression”	SUMO1	“transcriptional regulation”
PAK1	“down-regulates activity”	BCL6	phosphorylation
Gbeta	down-regulates	BCL6	phosphorylation
ERK1/2	down-regulates	BCL6	phosphorylation
PRKD2	“down-regulates activity”	BCL6	phosphorylation
MAPK1	down-regulates	BCL6	phosphorylation
MAPK3	down-regulates	BCL6	phosphorylation
BCL6	“down-regulates quantity by repression”	CD80	“transcriptional regulation”

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 73 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.

GO biological processes:

GO term	Partners	Fold	FDR
negative regulation of gene expression, epigenetic	5	32.4×	2e-04
proteasome-mediated ubiquitin-dependent protein catabolic process	9	7.6×	7e-04

Disease & clinical

Cancer significance

From intOGen — cancer-driver classification: activating (oncogene-like) across 2 cancer types — DLBCLNOS, MLYM.

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	0
Uncertain significance	57
Likely benign	6
Benign	4

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
57871	GRCh38/hg38 3q27.3-28(chr3:187446231-190839052)x1	Pathogenic

SpliceAI

1579 predictions. Top by Δscore:

Variant	Effect	Δscore
3:187722597:TCACA:T	acceptor_gain	1.0000
3:187722598:CACA:C	acceptor_gain	1.0000
3:187722598:CACAC:C	acceptor_gain	1.0000
3:187722599:ACA:A	acceptor_gain	1.0000
3:187722600:CA:C	acceptor_gain	1.0000
3:187722600:CAC:C	acceptor_gain	1.0000
3:187722602:C:CC	acceptor_gain	1.0000
3:187722605:C:CT	acceptor_gain	1.0000
3:187724936:CGTA:C	donor_gain	1.0000
3:187724938:TACAT:T	donor_loss	1.0000
3:187724939:A:AC	donor_gain	1.0000
3:187724940:C:CC	donor_gain	1.0000
3:187724940:CA:C	donor_gain	1.0000
3:187724940:CAT:C	donor_gain	1.0000
3:187724940:CATG:C	donor_gain	1.0000
3:187724956:T:A	donor_gain	1.0000
3:187725075:CCAC:C	acceptor_gain	1.0000
3:187725076:CAC:C	acceptor_gain	1.0000
3:187725076:CACC:C	acceptor_gain	1.0000
3:187725076:CACCT:C	acceptor_loss	1.0000
3:187725077:ACCTG:A	acceptor_loss	1.0000
3:187725078:CCT:C	acceptor_loss	1.0000
3:187725079:C:CC	acceptor_gain	1.0000
3:187725494:CTCA:C	donor_loss	1.0000
3:187725495:TCA:T	donor_loss	1.0000
3:187725497:A:AC	donor_gain	1.0000
3:187725497:ACC:A	donor_loss	1.0000
3:187725498:C:CC	donor_gain	1.0000
3:187725625:CTCAC:C	acceptor_gain	1.0000
3:187725626:TCACC:T	acceptor_gain	1.0000

AlphaMissense

4691 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
3:187722553:G:C	H676D	1.000
3:187722561:A:G	L673P	1.000
3:187722578:G:C	F667L	1.000
3:187722578:G:T	F667L	1.000
3:187722579:A:G	F667S	1.000
3:187722580:A:G	F667L	1.000
3:187722601:A:G	C660R	1.000
3:187724964:G:C	H652D	1.000
3:187724972:A:G	L649P	1.000
3:187724976:G:C	H648D	1.000
3:187724984:A:G	L645P	1.000
3:187725001:G:C	F639L	1.000
3:187725001:G:T	F639L	1.000
3:187725002:A:G	F639S	1.000
3:187725003:A:G	F639L	1.000
3:187725013:A:C	C635W	1.000
3:187725014:C:T	C635Y	1.000
3:187725022:A:C	C632W	1.000
3:187725024:A:G	C632R	1.000
3:187725068:A:G	L617P	1.000
3:187725505:A:C	F611L	1.000
3:187725505:A:T	F611L	1.000
3:187725506:A:G	F611S	1.000
3:187725507:A:G	F611L	1.000
3:187725517:G:C	C607W	1.000
3:187725518:C:T	C607Y	1.000
3:187725528:A:G	C604R	1.000
3:187725564:G:C	H592D	1.000
3:187725572:A:G	L589P	1.000
3:187725589:G:C	F583L	1.000

dbSNP variants (sampled 300 via entrez): RS1000020139 (3:187736717 C>A), RS1000083045 (3:187745356 AGCG>A,AGCGGCGGCG), RS1000122039 (3:187742795 T>C), RS1000363741 (3:187724754 G>A,T), RS1000754741 (3:187743033 T>A), RS1000859494 (3:187738461 G>A), RS1000948880 (3:187747338 T>C), RS1000960235 (3:187743456 A>C), RS1000999759 (3:187746940 C>T), RS1001142937 (3:187731262 C>T), RS1001196934 (3:187747447 G>C), RS1001246732 (3:187742493 T>G), RS1001344931 (3:187742086 A>G), RS1001351535 (3:187742229 T>C), RS1001408988 (3:187731614 G>A,C)

Disease associations

OMIM: gene MIM:109565 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

17 total (17 of 17 shown, HPO-id order):

HPO	Term
HP:0001004	Lymphedema
HP:0001287	Meningitis
HP:0001541	Ascites
HP:0001744	Splenomegaly
HP:0001824	Weight loss
HP:0001945	Fever
HP:0002202	Pleural effusion
HP:0002585	Abnormal peritoneum morphology
HP:0002665	Lymphoma
HP:0002716	Lymphadenopathy
HP:0003072	Hypercalcemia
HP:0012378	Fatigue
HP:0025435	Increased circulating lactate dehydrogenase concentration
HP:0030166	Night sweats
HP:0033823	Mediastinal mass
HP:0100721	Mediastinal lymphadenopathy
HP:0200036	Skin nodule

GWAS associations

26 associations (top):

Study	Trait	p-value
GCST001610_11	Renal function-related traits (BUN)	9.000000e-30
GCST001784_21	Pulmonary function (smoking interaction)	5.000000e-07
GCST001925_5	PR interval	6.000000e-06
GCST002066_1	B cell non-Hodgkin lymphoma	3.000000e-13
GCST002083_14	Self-reported allergy	1.000000e-09
GCST002084_4	Allergic sensitization	3.000000e-10
GCST002726_54	Glucose homeostasis traits	2.000000e-07
GCST002806_5	Type 2 diabetes	2.000000e-06
GCST003814_5	Selective IgA deficiency	3.000000e-07
GCST004608_81	Granulocyte percentage of myeloid white cells	4.000000e-09
GCST004631_60	Basophil percentage of white cells	7.000000e-11
GCST004634_20	Basophil percentage of granulocytes	3.000000e-12
GCST005038_33	Allergic disease (asthma, hay fever or eczema)	5.000000e-10
GCST005038_34	Allergic disease (asthma, hay fever or eczema)	1.000000e-08
GCST005986_35	Blood urea nitrogen levels	2.000000e-48
GCST008839_55	Height	4.000000e-16
GCST009028_36	Adverse response to drug	7.000000e-07
GCST009597_60	Multiple sclerosis	5.000000e-09
GCST009719_17	Allergic rhinitis	2.000000e-08
GCST009798_18	Asthma	2.000000e-09
GCST010244_429	Triglyceride levels	1.000000e-09
GCST90000025_682	Appendicular lean mass	3.000000e-10
GCST90002380_144	Basophil percentage of white cells	9.000000e-17
GCST90002394_265	Monocyte percentage of white cells	3.000000e-15
GCST90002399_409	Neutrophil percentage of white cells	3.000000e-10
GCST90020028_1699	Hip circumference adjusted for BMI	1.000000e-09

EFO canonical traits (14, from GWAS)

EFO ID	Trait name
EFO:0003892	pulmonary function measurement
EFO:0004713	FEV/FVC ratio
EFO:0004462	PR interval
EFO:0005298	allergic sensitization measurement
EFO:0006833	glucose effectiveness measurement
EFO:0007997	granulocyte percentage of myeloid white cells
EFO:0007992	basophil percentage of leukocytes
EFO:0007995	basophil percentage of granulocytes
EFO:0009658	adverse effect
EFO:0004530	triglyceride measurement
EFO:0004980	appendicular lean mass
EFO:0007989	monocyte percentage of leukocytes
EFO:0007990	neutrophil percentage of leukocytes
EFO:0008039	BMI-adjusted hip circumference

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (6): CHEMBL4105786 (SINGLE PROTEIN), CHEMBL4106125 (PROTEIN-PROTEIN INTERACTION), CHEMBL4523673 (PROTEIN-PROTEIN INTERACTION), CHEMBL4523692 (PROTEIN-PROTEIN INTERACTION), CHEMBL4523746 (PROTEIN-PROTEIN INTERACTION), CHEMBL6195567 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 881 (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
CHEMBL13589	AMANOZINE	2	482
CHEMBL1084546	PF-00562271	1	399

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: other protein — BTB (POZ) domain containing TFs

Most potent curated ligand interactions (6 total), top 6:

Ligand	Action	Affinity	Parameter
BI-3802	Binding	8.52	pIC50
JNJ-65234637	Binding	8.3	pKd
BCL6 PROTAC A19	Binding	7.89	pIC50
BCL6 PROTAC 15	Binding	6.92	pIC50
compound 8c [PMID: 28760529]	Binding	6.14	pIC50
FX1	Binding	5.15	pKd

Binding affinities (BindingDB)

151 measured of 407 human assays (407 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(2S)-10-[[5-chloro-2-(7-hydroxy-3-oxa-9-azabicyclo[3.3.1]nonan-9-yl)pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	IC50	1.17 nM	US-20230287003: BCL6 INHIBITORS
10-[[5-chloro-2-(7-hydroxy-3-oxa-9-azabicyclo[3.3.1]nonan-9-yl)pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	IC50	1.55 nM	US-20230287003: BCL6 INHIBITORS
9-[5-chloro-4-[[(2S)-2-cyclopropyl-3,3-difluoro-7-methyl-6-oxo-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-10-yl]amino]pyrimidin-2-yl]-N,N-dimethyl-3-oxa-9-azabicyclo[3.3.1]nonane-7-carboxamide	IC50	1.78 nM	US-20230287003: BCL6 INHIBITORS
(2S)-10-[[5-chloro-2-[(1S,5R)-3-methyl-2-oxo-3,8-diazabicyclo[3.2.1]octan-8-yl]pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	IC50	2.57 nM	US-20230287003: BCL6 INHIBITORS
(2R)-10-[[5-chloro-2-(7-hydroxy-3-oxa-9-azabicyclo[3.3.1]nonan-9-yl)pyrimidin-4-yl]amino]-2-cyclopropyl-7-methyl-1,2,3,4-tetrahydro-[1,4]oxazepino[2,3-c][1,8]naphthyridin-6-one	IC50	6.92 nM	US-20230287003: BCL6 INHIBITORS
(2R)-10-[[5-chloro-2-(7-hydroxy-3-oxa-9-azabicyclo[3.3.1]nonan-9-yl)pyrimidin-4-yl]amino]-2-cyclopropyl-7-methyl-1,2,3,4-tetrahydro-[1,4]thiazepino[2,3-c]quinolin-6-one	IC50	7.59 nM	US-20230287003: BCL6 INHIBITORS
(2R)-10-[[5-chloro-2-(7-hydroxy-3-oxa-9-azabicyclo[3.3.1]nonan-9-yl)pyrimidin-4-yl]amino]-2-cyclopropyl-7-methyl-1,2,3,4-tetrahydro-[1,4]oxazepino[2,3-c]quinolin-6-one	IC50	10.7 nM	US-20230287003: BCL6 INHIBITORS
(2R)-10-[[5-chloro-2-(3-hydroxy-8-azabicyclo[3.2.1]octan-8-yl)pyrimidin-4-yl]amino]-2-cyclopropyl-7-methyl-1,2,3,4-tetrahydro-[1,4]oxazepino[2,3-c]quinolin-6-one	IC50	11 nM	US-20230287003: BCL6 INHIBITORS
OICR 11029A	KD	11 nM
(2R)-10-[[5-chloro-2-(7-hydroxy-7-methyl-3-oxa-9-azabicyclo[3.3.1]nonan-9-yl)pyrimidin-4-yl]amino]-2-cyclopropyl-7-methyl-1,2,3,4-tetrahydro-[1,4]oxazepino[2,3-c]quinolin-6-one	IC50	11.7 nM	US-20230287003: BCL6 INHIBITORS
5-[7-[2-[[5-chloro-2-(8-methyl-3,8-diazabicyclo[3.2.1]octan-3-yl)-4-pyridinyl]amino]-2-oxoethyl]-3-methyl-4-oxopyrrolo[2,3-d]pyrimidin-5-yl]-3-fluoro-2-hydroxybenzamide	KD	16.7 nM	US-11518764: Substituted heteroaryls as inhibitors of the BCL6 BTB domain protein-protein interaction
(2R)-10-[[5-chloro-2-(2-oxa-6-azatricyclo[3.3.1.13,7]decan-6-yl)pyrimidin-4-yl]amino]-2-cyclopropyl-7-methyl-1,2,3,4-tetrahydro-[1,4]oxazepino[2,3-c]quinolin-6-one	IC50	22.9 nM	US-20230287003: BCL6 INHIBITORS
5-[7-[2-[[5-chloro-2-(2-oxa-5-azabicyclo[2.2.1]heptan-5-yl)-4-pyridinyl]amino]-2-oxoethyl]-3-methyl-4-oxopyrrolo[2,3-d]pyrimidin-5-yl]-3-fluoro-2-hydroxybenzamide	KD	23.4 nM	US-11518764: Substituted heteroaryls as inhibitors of the BCL6 BTB domain protein-protein interaction
5-[7-[2-[[2-(7-azabicyclo[2.2.1]heptan-7-yl)-5-chloro-4-pyridinyl]amino]-2-oxoethyl]-3-methyl-4-oxopyrrolo[2,3-d]pyrimidin-5-yl]-3-chloro-2-hydroxybenzamide	KD	30 nM	US-11518764: Substituted heteroaryls as inhibitors of the BCL6 BTB domain protein-protein interaction
2-((6-((5-chloro-2-(4- ((14-((2-(2,6- dioxopiperidin-3-yl)-1- oxoisoindolin-5-yl)oxy)- 3,6,9,12- tetraoxatetradecyl)oxy) piperidin-1-yl)pyrimidin- 4-yl)amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl)oxy)-N- methylacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
2-((6-((5-chloro-2-(4-((4- (2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin- 5-yl)piperazin-1- yl)methyl)piperidin-1- yl)pyrimidin-4- yl)amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl)oxy)-N- methylacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
(2S,4R)-N-(2-(4-((1-(5- chloro-4-((1-methyl-3-(2- (methylamino)-2- oxoethoxy)-2-oxo-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)piperidin-4- yl)oxy)butoxy)-4-(4- methylthiazol-5- yl)benzyl)-4-hydroxy-1- (3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine- 2-carboxamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
5-(4-(4-(5-chloro-4-((1- methyl-2-oxo-3-(2- oxopropoxy)-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)piperazin-1- yl)piperidin-1-yl)-2-(2,6- dioxopiperidin-3- yl)isoindoline-1,3-dione	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
5-(3-(4-(5-chloro-4-((1- methyl-2-oxo-3-(2- oxopropoxy)-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)piperazin-1- yl)piperidin-1-yl)-2-(2,6- dioxopiperidin-3- yl)isoindoline-1,3-dione	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
5-(4-(2-(1-(5-chloro-4- ((1-methyl-2-oxo-3-(2- oxopropoxy)-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)piperidin-4- yl)ethyl)piperazin-1-yl)- 2-(2,6-dioxopiperidin-3- yl)isoindoline-1,3-dione	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
5-(4-(4-(5-chloro-4-((1- methyl-2-oxo-3-(2- oxopropoxy)-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)piperazine-1- carbonyl)piperidin-1-yl)- 2-(2,6-dioxopiperidin-3- yl)isoindoline-1,3-dione	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
5-(3-(2-(1-(5-chloro-4- ((1-methyl-2-oxo-3-(2- oxopropoxy)-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)piperidin-4- yl)ethoxy)azetidin-1-yl)- 2-(2,6-dioxopiperidin-3- yl)isoindoline-1,3-dione	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
5-(6-((1-(5-chloro-4-((1- methyl-2-oxo-3-(2- oxopropoxy)-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)piperidin-4-yl)methyl)- 2,6 diazaspiro[3.3]heptan-2- yl)-2-(2,6-dioxopiperidin- 3-yl)isoindoline-1,3- dione	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
2-((6-((5-chloro-2-(3-((4- (1-(3-(2-(2,6- dioxopiperidin-3-yl)-1- oxoisoindolin-5-yl)prop- 2-yn-1-yl)piperidin-4- yl)phenoxy)methyl) piperidin-1-yl)pyrimidin- 4-yl)amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl)oxy)-N- methylacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
2-((6-((5-chloro-2-(4-(2- (2-(2-(3-((2-(2,6- dioxopiperidin-3-yl)-1- oxoisoindolin-5- yl)oxy)propoxy)ethoxy) ethoxy)ethoxy)piperidin- 1-yl)pyrimidin-4- yl)amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl)oxy)-N- methylacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
5-(4-((1-(5-chloro-4-((1- methyl-2-oxo-3-(2- oxopropoxy)-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)piperidin-4- yl)(methyl)amino) piperidin-1-yl)-2-(2,6- dioxopiperidin-3- yl)isoindoline-1,3-dione	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
5-(4-((1-(5-chloro-4-((1- methyl-2-oxo-3-(2- oxopropoxy)-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)piperidin-4- yl)oxy)piperidin-1-yl)-2- (2,6-dioxopiperidin-3- yl)isoindoline-1,3-dione	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
5-(4-((5-chloro-4-((1- methyl-2-oxo-3-(2- oxopropoxy)-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)ethynyl)piperidin-1- yl)-2-(2,6-dioxopiperidin- 3-yl)isoindoline-1,3- dione	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
(E)-3-(6-((5-chloro-2-(4- ((4-(2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-5- yl)piperazin-1- yl)methyl)piperidin-1- yl)pyrimidin-4- yl)amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl)-N- methylacrylamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
5-(3-((1-(5-chloro-4-((1- methyl-2-oxo-3-(2- oxopropoxy)-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)piperidin-4- yl)oxy)azetidin-1-yl)-2- (2,6-dioxopiperidin-3- yl)isoindoline-1,3-dione	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
5-(4-((1-(5-chloro-4-((1- methyl-2-oxo-3-(2- oxopropoxy)-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)azetidin-3- yl)oxy)piperidin-1-yl)-2- (2,6-dioxopiperidin-3- yl)isoindoline-1,3-dione	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
4-(4-((5-chloro-4-((1- methyl-2-oxo-3-(2- oxopropoxy)-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)ethynyl)piperidin-1- yl)-2-(2,6-dioxopiperidin- 3-yl)isoindoline-1,3- dione	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
2-((6-((5-chloro-2-(5-((1- (2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-5- yl)piperidin-4-yl)methyl)- 2,5-diazabicyclo [2.2.1]heptan- 2-yl)pyrimidin-4- yl)amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl)oxy)-N- methylacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
2-((6-((5-chloro-2-(4-((4- (2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-5- yl)-2-oxopiperazin-1- yl)methyl)piperidin-1- yl)pyrimidin-4- yl)amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl)oxy)-N- methylacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
5-(1’-((1-(5-chloro-4-((1- methyl-2-oxo-3-(2- oxopropoxy)-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)piperidin-4-yl)methyl)- [3,3’-biazetidin]-1-yl)-2- (2,6-dioxopiperidin-3- yl)isoindoline-1,3-dione	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
2-((6-((5-chloro-2-(4-(2- (4-(2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin- 5-yl)piperazin-1- yl)propan-2-yl)piperidin- 1-yl)pyrimidin-4- yl)amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl)oxy)-N- methylacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
2-((6-((5-chloro-2-(4-((4- (2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-5- yl)piperazin-1- yl)methyl)piperidin-1- yl)pyrimidin-4- yl)amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl)oxy)-N- methoxyacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
2-((6-((5-chloro-2-(4-((1- (2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-5- yl)piperidin-4-yl)methyl)- 1,4-diazepan-1- yl)pyrimidin-4- yl)amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl)oxy)-N- methylacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
5-(4-((1-(5-chloro-4-((1- methyl-2-oxo-3-(((R)-3- oxobutan-2-yl)oxy)-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)piperidin-4- yl)methyl)piperazin-1- yl)-2-((S)-2,6- dioxopiperidin-3- yl)isoindoline-1,3-dione	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
2-((6-((5-chloro-2-(4-(2- (4-(2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin- 5-yl)piperazin-1- yl)ethyl)piperazin-1- yl)pyrimidin-4- yl)amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl)oxy)-N- methylacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
2-((6-((5-chloro-2-(4-(3- (4-(2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin- 5-yl)piperazin-1- yl)propyl)piperazin-1- yl)pyrimidin-4- yl)amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl)oxy)-N- methylacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
5-(4-((4-(5-chloro-4-((1- methyl-3-(2- (methylamino)-2- oxoethoxy)-2-oxo-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)piperazin-1- yl)methyl)piperidin-1-yl)- N-(2,6-dioxopiperidin-3- yl)picolinamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
5-(4-(3-(4-(5-chloro-4- ((1-methyl-2-oxo-3-(2- oxopropoxy)-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)piperazin-1- yl)propyl)piperazin-1-yl)- 2-(2,6-dioxopiperidin-3- yl)isoindoline-1,3-dione	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
2-((6-((5-chloro-2-((3S)- 3-(((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-5- yl)oxy)methyl)piperidin- 1-yl)pyrimidin-4- yl)amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl)oxy)-N- methylacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
2-((6-((5-chloro-2-(4-((1- (2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-5- yl)-4-hydroxypiperidin-4- yl)methyl)piperazin-1- yl)pyrimidin-4- yl)amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl)oxy)-N- methylacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
2-((6-((5-chloro-2-(4-((1- (2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-5- yl)piperidin-4- yl)oxy)azepan-1- yl)pyrimidin-4- yl)amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl)oxy)-N- methylacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
5-(4-(2-(4-(5-chloro-4- ((1-methyl-2-oxo-3-(2- oxopropoxy)-1,2- dihydroquinolin-6- yl)amino)pyrimidin-2- yl)piperazin-1-yl)propan- 2-yl)piperidin-1-yl)-2- (2,6-dioxopiperidin-3- yl)isoindoline-1,3-dione	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
2-((6-((5-chloro-2-(4-((4- (2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4- yl)piperazin-1- yl)methyl)piperidin-1- yl)pyrimidin-4- yl)amino)-1-methyl-2- oxo-1,2-dihydroquinolin- 3-yl)oxy)-N- methylacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
2-((6-((5-chloro-2-(4-((1- (2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-5- yl)piperidin-4- yl)methyl)piperazin-1- yl)pyrimidin-4- yl)amino)-1-isopropyl-2- oxo-1,2-dihydroquinolin- 3-yl)oxy)-N- methylacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use
2-((6-((5-chloro-2-(4-(2- (1-(2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin- 5-yl)piperidin-4- yl)propan-2-yl)piperazin- 1-yl)pyridin-4-yl)amino)- 1-methyl-2-oxo-1,2- dihydroquinolin-3- yl)oxy)-N- methoxyacetamide	IC50	30 nM	US-12310975: Modulators of BCL6 proteolysis and associated methods of use

ChEMBL bioactivities

787 potent at pChembl≥5 of 856 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.30	Kd	0.5	nM	CHEMBL5282647
9.28	Kd	0.53	nM	CHEMBL5282647
9.24	Kd	0.57	nM	CHEMBL4077626
9.22	Kd	0.6	nM	CHEMBL5195604
9.15	EC50	0.7	nM	CHEMBL5205388
9.15	Kd	0.7	nM	CHEMBL5814333
9.11	Kd	0.77	nM	CHEMBL5834831
9.09	Kd	0.81	nM	CHEMBL5802828
9.06	IC50	0.87	nM	CHEMBL4084806
9.06	Kd	0.87	nM	CHEMBL5923367
9.05	IC50	0.9	nM	CHEMBL5396792
9.02	Kd	0.96	nM	CHEMBL5849108
9.02	Kd	0.96	nM	CHEMBL5978380
9.00	IC50	1	nM	CHEMBL4077626
9.00	Kd	1	nM	CHEMBL5195604
9.00	EC50	1	nM	CHEMBL5205388
9.00	Kd	1	nM	CHEMBL5270031
9.00	Kd	1	nM	CHEMBL5283745
8.89	IC50	1.3	nM	CHEMBL5394661
8.88	Kd	1.33	nM	CHEMBL5848081
8.87	Kd	1.36	nM	CHEMBL5876992
8.85	IC50	1.4	nM	CHEMBL5396893
8.85	Kd	1.42	nM	CHEMBL5838489
8.82	IC50	1.5	nM	CHEMBL4090962
8.82	IC50	1.5	nM	CHEMBL5204505
8.82	Kd	1.5	nM	CHEMBL5904511
8.81	Kd	1.55	nM	CHEMBL6047968
8.79	Kd	1.61	nM	CHEMBL5834405
8.77	IC50	1.7	nM	CHEMBL4066850
8.75	Kd	1.79	nM	CHEMBL5803625
8.72	IC50	1.9	nM	CHEMBL5427058
8.69	Kd	2.03	nM	CHEMBL6037729
8.67	Kd	2.14	nM	CHEMBL6038920
8.66	IC50	2.2	nM	CHEMBL5205388
8.66	EC50	2.2	nM	CHEMBL5205212
8.62	IC50	2.4	nM	CHEMBL4093418
8.60	IC50	2.5	nM	CHEMBL5171519
8.59	Kd	2.569	nM	CHEMBL4755229
8.57	EC50	2.7	nM	CHEMBL5204505
8.55	Kd	2.79	nM	CHEMBL5984561
8.54	IC50	2.9	nM	CHEMBL4094351
8.54	IC50	2.9	nM	CHEMBL5194697
8.54	IC50	2.9	nM	CHEMBL5196650
8.52	IC50	3	nM	CHEMBL4755229
8.52	IC50	3	nM	CHEMBL4795171
8.52	IC50	3	nM	CHEMBL5181921
8.52	Kd	3	nM	CHEMBL5285804
8.52	IC50	3	nM	CHEMBL5423054
8.52	Kd	3.02	nM	CHEMBL6046767
8.50	Kd	3.13	nM	CHEMBL5878795

PubChem BioAssay actives

527 with measured affinity, of 1115 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
7-[6-[2-[[3-chloro-6-[(2S)-2,4-dimethylpiperazin-1-yl]-2-fluoro-4-pyridinyl]amino]-2-oxoethyl]-2-oxo-1,6,8-triazatricyclo[7.3.0.03,7]dodeca-3(7),4,8-trien-4-yl]-4-hydroxy-1,3-benzodioxole-5-carboxamide	1920225: Surface Plasmon Resonance (SPR) assay from Article 10.1021/acsmedchemlett.2c00502: “Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.”	kd	0.0005	uM
(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-3-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carboxylic acid	1462114: Binding affinity to biotinylated BCL6 (unknown origin) by SPR analysis	kd	0.0006	uM
(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-3-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carboxylic acid	1897155: Binding affinity to BCL6 BTB domain (unknown origin) by SPR analysis	kd	0.0006	uM
(2S)-10-[[5-chloro-2-[(3R,5S)-3-hydroxy-5-methylpiperidin-1-yl]pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1911987: Degradation of BCL6 in human OCI-Ly1 cells incubated for 2 hrs by MSD assay	ec50	0.0007	uM
(12S,14S,17E)-7-chloro-12-(hydroxymethyl)-23-(3-morpholin-4-ylpropyl)-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-24-one	1447965: Inhibition of SMRT2 H1426W mutant peptide binding to N-terminal His6-tagged human BCL6 BTB domain C8Q/C67R/C84N mutant expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by SMRT2 H1426W mutant peptide addition measured after 60 mins by time-resolved fluorescence resonance energy transfer assay	ic50	0.0009	uM
(2S)-10-[[2-(3-acetyl-3,8-diazabicyclo[3.2.1]octan-8-yl)-5-chloropyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1987509: Inhibition of N-terminal Trx/6His/HRV3C-tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI using RSEIISTAPSSWVVPGP-Cys-AlexaFluor 633-amide as substrate measured after 2 hrs by TR-FRET assay	ic50	0.0009	uM
7-[7-[2-[[3-chloro-6-[(2S)-2,4-dimethylpiperazin-1-yl]-2-fluoro-4-pyridinyl]amino]-2-oxoethyl]-2,3-dimethyl-4-oxopyrrolo[2,3-d]pyrimidin-5-yl]-4-hydroxy-1,3-benzodioxole-5-carboxamide	1920225: Surface Plasmon Resonance (SPR) assay from Article 10.1021/acsmedchemlett.2c00502: “Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.”	kd	0.0010	uM
7-[7-[2-[[3-chloro-6-[(2S)-2,4-dimethylpiperazin-1-yl]-2-fluoro-4-pyridinyl]amino]-2-oxoethyl]-3-methyl-4-oxopyrrolo[2,3-d]pyrimidin-5-yl]-4-hydroxy-1,3-benzodioxole-5-carboxamide	1920225: Surface Plasmon Resonance (SPR) assay from Article 10.1021/acsmedchemlett.2c00502: “Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.”	kd	0.0010	uM
(2S)-10-[[5-chloro-2-[(1S,5R)-7-hydroxy-3-oxa-9-azabicyclo[3.3.1]nonan-9-yl]pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1987509: Inhibition of N-terminal Trx/6His/HRV3C-tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI using RSEIISTAPSSWVVPGP-Cys-AlexaFluor 633-amide as substrate measured after 2 hrs by TR-FRET assay	ic50	0.0013	uM
(2S)-10-[[5-chloro-2-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1987509: Inhibition of N-terminal Trx/6His/HRV3C-tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI using RSEIISTAPSSWVVPGP-Cys-AlexaFluor 633-amide as substrate measured after 2 hrs by TR-FRET assay	ic50	0.0014	uM
(12S,14S,17E)-7-chloro-12-(hydroxymethyl)-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-24-one	1447965: Inhibition of SMRT2 H1426W mutant peptide binding to N-terminal His6-tagged human BCL6 BTB domain C8Q/C67R/C84N mutant expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by SMRT2 H1426W mutant peptide addition measured after 60 mins by time-resolved fluorescence resonance energy transfer assay	ic50	0.0015	uM
(2S)-10-[[5-chloro-2-[(3R)-4,4-difluoro-3-(hydroxymethyl)piperidin-1-yl]pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1911986: Inhibition of N-terminal thioredoxin-His6 tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI incubated for 2 hrs by TR-FRET assay	ic50	0.0015	uM
2-[(12S,14S,17E)-7-cyano-24-oxo-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-12-yl]acetic acid	1447965: Inhibition of SMRT2 H1426W mutant peptide binding to N-terminal His6-tagged human BCL6 BTB domain C8Q/C67R/C84N mutant expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by SMRT2 H1426W mutant peptide addition measured after 60 mins by time-resolved fluorescence resonance energy transfer assay	ic50	0.0017	uM
(2S)-10-[[2-(8-acetyl-3,8-diazabicyclo[3.2.1]octan-3-yl)-5-chloropyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1987509: Inhibition of N-terminal Trx/6His/HRV3C-tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI using RSEIISTAPSSWVVPGP-Cys-AlexaFluor 633-amide as substrate measured after 2 hrs by TR-FRET assay	ic50	0.0019	uM
N-[(3R,5S)-1-[5-chloro-4-[[(2S)-2-cyclopropyl-3,3-difluoro-7-methyl-6-oxo-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-10-yl]amino]pyrimidin-2-yl]-5-methylpiperidin-3-yl]acetamide	1911987: Degradation of BCL6 in human OCI-Ly1 cells incubated for 2 hrs by MSD assay	ec50	0.0022	uM
(12S,14S)-12-(hydroxymethyl)-24-oxo-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,21(29),22(27)-heptaene-7-carbonitrile	1447965: Inhibition of SMRT2 H1426W mutant peptide binding to N-terminal His6-tagged human BCL6 BTB domain C8Q/C67R/C84N mutant expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by SMRT2 H1426W mutant peptide addition measured after 60 mins by time-resolved fluorescence resonance energy transfer assay	ic50	0.0024	uM
(2S)-10-[[5-chloro-2-[(3S)-3-hydroxypiperidin-1-yl]pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1911986: Inhibition of N-terminal thioredoxin-His6 tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI incubated for 2 hrs by TR-FRET assay	ic50	0.0025	uM
(12S,14S,17E)-12-(hydroxymethyl)-24-oxo-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaene-7-carbonitrile	1447965: Inhibition of SMRT2 H1426W mutant peptide binding to N-terminal His6-tagged human BCL6 BTB domain C8Q/C67R/C84N mutant expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by SMRT2 H1426W mutant peptide addition measured after 60 mins by time-resolved fluorescence resonance energy transfer assay	ic50	0.0029	uM
(2S)-10-[[5-chloro-2-[(3S,5R)-3-hydroxy-5-methylpiperidin-1-yl]pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1911986: Inhibition of N-terminal thioredoxin-His6 tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI incubated for 2 hrs by TR-FRET assay	ic50	0.0029	uM
N-[(3S,5R)-1-[5-chloro-4-[[(2S)-2-cyclopropyl-3,3-difluoro-7-methyl-6-oxo-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-10-yl]amino]pyrimidin-2-yl]-5-methylpiperidin-3-yl]acetamide	1911986: Inhibition of N-terminal thioredoxin-His6 tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI incubated for 2 hrs by TR-FRET assay	ic50	0.0029	uM
2-[6-[[5-chloro-2-[(3S,5R)-3,5-dimethylpiperidin-1-yl]pyrimidin-4-yl]amino]-1-methyl-2-oxoquinolin-3-yl]oxy-N-methylacetamide	2067053: Inhibition of BCL6 BTB domain (5 to 129 residues) (unknown origin) expressed in Escherichia coli using 5-TAMRA-RSEIISTAPSSWVVPGP as substrate incubated 1 hr by TR-FRET assay	ic50	0.0030	uM
1-[5-chloro-4-[[8-methoxy-1-methyl-3-[2-(methylamino)-2-oxoethoxy]-2-oxoquinolin-6-yl]amino]pyrimidin-2-yl]-N,N-dimethylpiperidine-4-carboxamide	1673914: Inhibition of BCOR peptide binding to BCL6 BTB domain (5 to 129 residues) C8Q/C67R/C84N triple mutant (unknown origin) expressed in Escherichia coli BL21(DE3) cells preincubated for 30 mins followed by BCOR ULight peptide addition and measured after 240 mins by TR-FRET assay	ic50	0.0030	uM
2-[6-[[5-chloro-2-[(3S,5R)-3,5-dimethylpiperidin-1-yl]pyrimidin-4-yl]amino]-8-methoxy-1-methyl-2-oxoquinolin-3-yl]oxy-N-methylacetamide	1673914: Inhibition of BCOR peptide binding to BCL6 BTB domain (5 to 129 residues) C8Q/C67R/C84N triple mutant (unknown origin) expressed in Escherichia coli BL21(DE3) cells preincubated for 30 mins followed by BCOR ULight peptide addition and measured after 240 mins by TR-FRET assay	ic50	0.0030	uM
2-chloro-4-[[4-[2-(5-cyclopropylpyrimidin-2-yl)propan-2-ylamino]-1-methyl-2-oxoquinolin-6-yl]amino]pyridine-3-carbonitrile	1833927: Inhibition of BCOR peptide binding to human BCL6 expressed in Escherichia coli measured after 270 mins by BCOR ULight TR-FRET assay	ic50	0.0030	uM
5-[7-[2-[[3-chloro-6-[(2S)-2,4-dimethylpiperazin-1-yl]-2-fluoro-4-pyridinyl]amino]-2-oxoethyl]-3-methyl-4-oxopyrrolo[2,3-d]pyrimidin-5-yl]-3-fluoro-2-hydroxybenzamide	1920225: Surface Plasmon Resonance (SPR) assay from Article 10.1021/acsmedchemlett.2c00502: “Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.”	kd	0.0030	uM
(2S)-10-[[5-chloro-2-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1987509: Inhibition of N-terminal Trx/6His/HRV3C-tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI using RSEIISTAPSSWVVPGP-Cys-AlexaFluor 633-amide as substrate measured after 2 hrs by TR-FRET assay	ic50	0.0030	uM
(2S)-10-[[5-chloro-2-[(3R)-3-hydroxypiperidin-1-yl]pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1911986: Inhibition of N-terminal thioredoxin-His6 tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI incubated for 2 hrs by TR-FRET assay	ic50	0.0030	uM
(2S)-10-[(5-chloro-2-morpholin-4-ylpyrimidin-4-yl)amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1987509: Inhibition of N-terminal Trx/6His/HRV3C-tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI using RSEIISTAPSSWVVPGP-Cys-AlexaFluor 633-amide as substrate measured after 2 hrs by TR-FRET assay	ic50	0.0032	uM
(12S,14S)-7-chloro-12-(hydroxymethyl)-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,21(29),22(27)-heptaen-24-one	1447965: Inhibition of SMRT2 H1426W mutant peptide binding to N-terminal His6-tagged human BCL6 BTB domain C8Q/C67R/C84N mutant expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by SMRT2 H1426W mutant peptide addition measured after 60 mins by time-resolved fluorescence resonance energy transfer assay	ic50	0.0033	uM
(2S)-10-[[5-chloro-2-[(3R,5S)-3-(dimethylamino)-5-methylpiperidin-1-yl]pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1911986: Inhibition of N-terminal thioredoxin-His6 tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI incubated for 2 hrs by TR-FRET assay	ic50	0.0033	uM
(2S)-10-[[5-chloro-2-[(3S)-4,4-difluoro-3-hydroxypiperidin-1-yl]pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1911986: Inhibition of N-terminal thioredoxin-His6 tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI incubated for 2 hrs by TR-FRET assay	ic50	0.0035	uM
(2S)-10-[[5-chloro-2-[(3S,5R)-3-(dimethylamino)-5-methylpiperidin-1-yl]pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1911986: Inhibition of N-terminal thioredoxin-His6 tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI incubated for 2 hrs by TR-FRET assay	ic50	0.0036	uM
(2S)-10-[[5-chloro-2-(3-methoxyazetidin-1-yl)pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1987509: Inhibition of N-terminal Trx/6His/HRV3C-tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI using RSEIISTAPSSWVVPGP-Cys-AlexaFluor 633-amide as substrate measured after 2 hrs by TR-FRET assay	ic50	0.0037	uM
2-chloro-4-[[(2S)-2-cyclopropyl-3,3-difluoro-7-methyl-6-oxo-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-10-yl]amino]pyridine-3-carbonitrile	1880506: Inhibition of human N-terminal thioredoxin 6-His tagged BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI using BCOR-AF633 peptide as substrate incubated for 2 hrs by TR-FRET assay	ic50	0.0039	uM
(2S)-10-[[5-chloro-2-[(3S)-4,4-difluoro-3-(hydroxymethyl)piperidin-1-yl]pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1911986: Inhibition of N-terminal thioredoxin-His6 tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI incubated for 2 hrs by TR-FRET assay	ic50	0.0041	uM
(2S)-10-[[5-chloro-2-[(3R)-4,4-difluoro-3-hydroxypiperidin-1-yl]pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1911986: Inhibition of N-terminal thioredoxin-His6 tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI incubated for 2 hrs by TR-FRET assay	ic50	0.0046	uM
(12S,14S,17E)-7-chloro-12-(hydroxymethyl)-23-methyl-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-24-one	1447965: Inhibition of SMRT2 H1426W mutant peptide binding to N-terminal His6-tagged human BCL6 BTB domain C8Q/C67R/C84N mutant expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by SMRT2 H1426W mutant peptide addition measured after 60 mins by time-resolved fluorescence resonance energy transfer assay	ic50	0.0049	uM
(12S,14S,17E)-7-chloro-23-[(3,3-difluorocyclobutyl)methyl]-12-(hydroxymethyl)-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-24-one	1447965: Inhibition of SMRT2 H1426W mutant peptide binding to N-terminal His6-tagged human BCL6 BTB domain C8Q/C67R/C84N mutant expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by SMRT2 H1426W mutant peptide addition measured after 60 mins by time-resolved fluorescence resonance energy transfer assay	ic50	0.0050	uM
5-[6-[2-[[3-chloro-6-[(2S)-2,4-dimethylpiperazin-1-yl]-2-fluoro-4-pyridinyl]amino]-2-oxoethyl]-2-oxo-1,6,8-triazatricyclo[7.3.0.03,7]dodeca-3(7),4,8-trien-4-yl]-3,4-difluoro-2-hydroxybenzamide	1920225: Surface Plasmon Resonance (SPR) assay from Article 10.1021/acsmedchemlett.2c00502: “Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.”	kd	0.0050	uM
1-[5-chloro-4-[[(2S)-2-cyclopropyl-3,3-difluoro-7-methyl-6-oxo-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-10-yl]amino]pyrimidin-2-yl]azetidine-3-carbonitrile	1987509: Inhibition of N-terminal Trx/6His/HRV3C-tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI using RSEIISTAPSSWVVPGP-Cys-AlexaFluor 633-amide as substrate measured after 2 hrs by TR-FRET assay	ic50	0.0050	uM
(2S)-10-[[2-(azetidin-1-yl)-5-chloropyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1987509: Inhibition of N-terminal Trx/6His/HRV3C-tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI using RSEIISTAPSSWVVPGP-Cys-AlexaFluor 633-amide as substrate measured after 2 hrs by TR-FRET assay	ic50	0.0055	uM
(2S)-10-[[5-chloro-2-(3-fluoroazetidin-1-yl)pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1987509: Inhibition of N-terminal Trx/6His/HRV3C-tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI using RSEIISTAPSSWVVPGP-Cys-AlexaFluor 633-amide as substrate measured after 2 hrs by TR-FRET assay	ic50	0.0057	uM
3-chloro-5-[7-[2-[[3-chloro-6-[(2S)-2,4-dimethylpiperazin-1-yl]-2-fluoro-4-pyridinyl]amino]-2-oxoethyl]-3-methyl-4-oxopyrrolo[2,3-d]pyrimidin-5-yl]-2-hydroxybenzamide	1920226: Surface Plasmon Resonance (SPR) assay from OICR from Article 10.1021/acsmedchemlett.2c00502: “Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.”	kd	0.0060	uM
(2S)-10-[(3-chloro-2-fluoro-4-pyridinyl)amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1987509: Inhibition of N-terminal Trx/6His/HRV3C-tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI using RSEIISTAPSSWVVPGP-Cys-AlexaFluor 633-amide as substrate measured after 2 hrs by TR-FRET assay	ic50	0.0060	uM
(2S)-10-[[5-chloro-2-[(3S,5S)-3-hydroxy-5-methylpiperidin-1-yl]pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1911986: Inhibition of N-terminal thioredoxin-His6 tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI incubated for 2 hrs by TR-FRET assay	ic50	0.0060	uM
(2S)-10-[[5-chloro-2-[(3S)-3-methylpiperidin-1-yl]pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1911987: Degradation of BCL6 in human OCI-Ly1 cells incubated for 2 hrs by MSD assay	ec50	0.0063	uM
(13R)-4-chloro-5-fluoro-11,21-dimethyl-15,18-dioxa-2,6,8,11,21,28-hexazapentacyclo[17.7.1.13,7.08,13.020,25]octacosa-1(26),3,5,7(28),19(27),20(25)-hexaen-22-one	1897197: Binding affinity to BCL6 (unknown origin) by TR-FRET assay	ic50	0.0089	uM
(12S,14S,17E)-7-chloro-12-(hydroxymethyl)-23-(pyridin-4-ylmethyl)-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-24-one	1447965: Inhibition of SMRT2 H1426W mutant peptide binding to N-terminal His6-tagged human BCL6 BTB domain C8Q/C67R/C84N mutant expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by SMRT2 H1426W mutant peptide addition measured after 60 mins by time-resolved fluorescence resonance energy transfer assay	ic50	0.0099	uM
(2S)-10-[[5-chloro-2-[(3R,5R)-3-hydroxy-5-methylpiperidin-1-yl]pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one	1911986: Inhibition of N-terminal thioredoxin-His6 tagged human BCL6 BTB domain (5 to 129 residues) expressed in Escherichia coli BL21-AI incubated for 2 hrs by TR-FRET assay	ic50	0.0099	uM
3-chloro-5-[7-[2-[(5-chloro-2-morpholin-4-yl-4-pyridinyl)amino]-2-oxoethyl]-3-methyl-4-oxopyrrolo[2,3-d]pyrimidin-5-yl]-2-hydroxybenzamide	1920226: Surface Plasmon Resonance (SPR) assay from OICR from Article 10.1021/acsmedchemlett.2c00502: “Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.”	kd	0.0100	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Particulate Matter	increases expression, affects cotreatment, affects expression, increases reaction, decreases expression (+1 more)	5
(+)-JQ1 compound	affects binding, decreases reaction, decreases expression, increases expression	4
Air Pollutants	increases abundance, decreases expression, increases expression, affects expression	4
Tetrachlorodibenzodioxin	decreases reaction, increases expression, affects reaction, affects binding, increases reaction (+2 more)	4
Cadmium Chloride	decreases expression, increases abundance, increases expression	4
Resveratrol	decreases expression, increases expression	3
Benzo(a)pyrene	affects methylation, decreases expression, increases expression	3
Cisplatin	affects expression, affects cotreatment, increases expression	3
Ozone	increases expression, affects expression, increases abundance, affects cotreatment, decreases expression	3
sulforaphane	decreases expression, increases expression	2
sodium arsenite	decreases expression, increases expression	2
Arsenic	affects methylation, increases expression, increases reaction	2
Cadmium	decreases expression, increases abundance, increases expression	2
Doxorubicin	decreases expression, increases expression	2
Estradiol	decreases expression, affects cotreatment	2
Formaldehyde	increases expression	2
Hydrogen Peroxide	affects expression, increases expression	2
Phenylmercuric Acetate	affects cotreatment, increases expression	2
Smoke	increases abundance, decreases expression	2
Cyclosporine	decreases expression	2
p-Chloromercuribenzoic Acid	affects cotreatment, increases expression	2
aristolochic acid I	increases expression	1
3-((6-(2-methoxyphenyl)pyrimidin-4-yl)amino)phenyl)methane sulfonamide	decreases expression	1
FR900359	increases phosphorylation	1
dicrotophos	increases expression	1
ethylbenzene	increases expression	1
methylmercuric chloride	increases expression	1
triphenyl phosphate	affects expression	1
bisphenol A	decreases expression, increases methylation	1
deoxynivalenol	increases expression	1

ChEMBL screening assays

209 unique, capped per target: 202 binding, 7 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4015777	Binding	Inhibition of SMRT peptide binding to 15N-labeled human BCL6 BTB domain C8Q/C67R/C84N mutant expressed in Escherichia coli BL21 by 2D-NMR method	Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors. — J Med Chem
CHEMBL5059389	Functional	Proliferation assay (SUDHL-4 cells)	Data for DCP probe CCT369260

Cellosaurus cell lines

14 cell lines: 11 cancer cell line, 3 embryonic stem cell

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

Cellosaurus	Name	Category	Sex
CVCL_1163	D-538MG	Cancer cell line
CVCL_1822	Karpas-231	Cancer cell line	Female
CVCL_A0H8	SEES3-1V human BCL6, clone1	Embryonic stem cell	Male
CVCL_A0H9	SEES3-1V human BCL6, clone2	Embryonic stem cell	Male
CVCL_A0I0	SEES3-1V human BCL6, clone3	Embryonic stem cell	Male
CVCL_B1L6	Abcam HeLa BCL6 KO	Cancer cell line	Female
CVCL_B8BZ	Abcam HCT 116 BCL6 KO	Cancer cell line	Male
CVCL_B8SY	Abcam MCF-7 BCL6 KO	Cancer cell line	Female
CVCL_B9E3	Abcam A-549 BCL6 KO	Cancer cell line	Male
CVCL_IU39	YM	Cancer cell line	Male

Clinical trials (associated diseases)

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