BCL2L1

gene

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Also known as BCLXBCL2LBcl-Xbcl-xLbcl-xSPPP1R52

Summary

BCL2L1 (BCL2 like 1, HGNC:992) is a protein-coding gene on chromosome 20q11.21, encoding Bcl-2-like protein 1 (Q07817). Potent inhibitor of cell death. It is a selective cancer dependency (DepMap: 86.5% of cell lines).

The protein encoded by this gene belongs to the BCL-2 protein family. BCL-2 family members form hetero- or homodimers and act as anti- or pro-apoptotic regulators that are involved in a wide variety of cellular activities. The proteins encoded by this gene are located at the outer mitochondrial membrane, and have been shown to regulate outer mitochondrial membrane channel (VDAC) opening. VDAC regulates mitochondrial membrane potential, and thus controls the production of reactive oxygen species and release of cytochrome C by mitochondria, both of which are the potent inducers of cell apoptosis. Alternative splicing results in multiple transcript variants encoding two different isoforms. The longer isoform acts as an apoptotic inhibitor and the shorter isoform acts as an apoptotic activator.

Source: NCBI Gene 598 — RefSeq curated summary.

At a glance

GWAS associations: 15
Clinical variants (ClinVar): 17 total
Druggable target: yes — 13 molecules with ChEMBL bioactivity
Cancer dependency (DepMap): dependent in 86.5% of screened cell lines
MANE Select transcript: NM_138578

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:992
Approved symbol	BCL2L1
Name	BCL2 like 1
Location	20q11.21
Locus type	gene with protein product
Status	Approved
Aliases	BCLX, BCL2L, Bcl-X, bcl-xL, bcl-xS, PPP1R52
Ensembl gene	ENSG00000171552
Ensembl biotype	protein_coding
OMIM	600039
Entrez	598

Gene structure

Transcript identifiers

Ensembl transcripts: 33 — 31 protein_coding, 1 protein_coding_CDS_not_defined, 1 nonsense_mediated_decay

ENST00000307677, ENST00000376055, ENST00000376062, ENST00000420488, ENST00000422920, ENST00000434194, ENST00000439267, ENST00000450273, ENST00000456404, ENST00000676582, ENST00000676942, ENST00000677194, ENST00000677494, ENST00000678563, ENST00000678671, ENST00000870614, ENST00000870615, ENST00000870616, ENST00000870617, ENST00000870618, ENST00000870619, ENST00000870620, ENST00000870621, ENST00000870622, ENST00000870623, ENST00000925012, ENST00000925013, ENST00000925014, ENST00000925015, ENST00000925016, ENST00000925017, ENST00000941693, ENST00000941694

RefSeq mRNA: 10 — MANE Select: NM_138578 NM_001191, NM_001317919, NM_001317920, NM_001317921, NM_001322239, NM_001322240, NM_001322242, NM_001424331, NM_001424332, NM_138578

CCDS: CCDS13188, CCDS13189

Canonical transcript exons

ENST00000307677 — 3 exons

Exon	Start	End
ENSE00001929365	31722618	31722868
ENSE00003788543	31721655	31722348
ENSE00003844866	31664458	31666086

Expression profiles

Bgee: expression breadth ubiquitous, 284 present calls, max score 97.46.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 86.1157 / max 4610.4961, expressed in 1824 samples.

FANTOM5 promoters (32 alternative TSS)

Promoter ID	TPM avg	Samples expressed
186863	26.8283	1775
186872	12.7908	1790
186862	8.8430	1590
186864	8.4466	1621
186870	7.9354	1730
186859	6.7449	949
186860	2.5227	879
186857	2.2023	569
186867	1.5774	454
186851	1.4815	825

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right lung	UBERON:0002167	97.46	gold quality
lower esophagus mucosa	UBERON:0035834	97.33	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	97.22	gold quality
upper lobe of left lung	UBERON:0008952	97.17	gold quality
metanephros cortex	UBERON:0010533	97.17	gold quality
descending thoracic aorta	UBERON:0002345	96.84	gold quality
ascending aorta	UBERON:0001496	96.76	gold quality
thoracic aorta	UBERON:0001515	96.76	gold quality
right coronary artery	UBERON:0001625	96.67	gold quality
islet of Langerhans	UBERON:0000006	96.55	gold quality
monocyte	CL:0000576	96.54	gold quality
left coronary artery	UBERON:0001626	96.54	gold quality
gall bladder	UBERON:0002110	96.52	gold quality
upper lobe of lung	UBERON:0008948	96.46	gold quality
aorta	UBERON:0000947	96.36	gold quality
coronary artery	UBERON:0001621	96.26	gold quality
mononuclear cell	CL:0000842	96.18	gold quality
popliteal artery	UBERON:0002250	96.14	gold quality
tibial artery	UBERON:0007610	96.13	gold quality
apex of heart	UBERON:0002098	95.92	gold quality
leukocyte	CL:0000738	95.91	gold quality
tibial nerve	UBERON:0001323	95.53	gold quality
minor salivary gland	UBERON:0001830	95.51	gold quality
body of stomach	UBERON:0001161	95.29	gold quality
right frontal lobe	UBERON:0002810	95.23	gold quality
esophagus mucosa	UBERON:0002469	95.14	gold quality
blood	UBERON:0000178	95.10	gold quality
esophagus	UBERON:0001043	94.91	gold quality
skin of leg	UBERON:0001511	94.84	gold quality
ganglionic eminence	UBERON:0004023	94.81	gold quality

Single-cell (SCXA)

Detected in 7 experiment(s), a significant marker in 5.

Experiment	Marker?	Max mean expression
E-MTAB-10042	yes	25.34
E-MTAB-9221	yes	22.83
E-HCAD-9	yes	6.04
E-HCAD-10	yes	3.31
E-GEOD-99795	no	185.62
E-MTAB-9467	no	1.91
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AP1, AR, BCL6, CD27, CD40, CD79A, CEBPB, CREB1, CTNNB1, EGR3, ENO1, ESR1, ETS1, ETS2, ETV6, EWSR1, FLI1, FLT3, FOS, FOXC1, FOXO1, GATA1, GATA3, GATA4, GFI1B, HIF1A, ID2, IKZF1, IRF2, IRF8, JUN, KLF11, KLF6, MTA1, MYB, MYC, MYOD1, NFE2L2, NFIL3, NFKB1

miRNA regulators (miRDB)

133 targeting BCL2L1, 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-4533	100.00	69.48	2758
HSA-MIR-518D-5P	100.00	67.51	979
HSA-MIR-518E-5P	100.00	67.66	954
HSA-MIR-518F-5P	100.00	67.51	979
HSA-MIR-519A-5P	100.00	67.66	954
HSA-MIR-519B-5P	100.00	67.66	954
HSA-MIR-519C-5P	100.00	67.66	954
HSA-MIR-520C-5P	100.00	67.51	979
HSA-MIR-522-5P	100.00	67.66	954
HSA-MIR-523-5P	100.00	67.66	954
HSA-MIR-526A-5P	100.00	67.51	979
HSA-MIR-4283	100.00	66.42	2097
HSA-MIR-10401-5P	99.99	65.79	948
HSA-MIR-513B-5P	99.99	69.96	2150
HSA-MIR-4500	99.99	72.72	2367
HSA-LET-7A-5P	99.98	72.29	1790
HSA-LET-7B-5P	99.98	72.31	1790
HSA-LET-7C-5P	99.98	72.29	1790
HSA-LET-7E-5P	99.98	72.29	1790
HSA-LET-7F-5P	99.98	72.56	1784
HSA-LET-7G-5P	99.98	72.37	1784
HSA-LET-7I-5P	99.98	72.37	1788
HSA-MIR-98-5P	99.98	72.33	1787
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-495-3P	99.96	72.81	4197
HSA-MIR-5688	99.96	73.23	4504
HSA-MIR-4725-3P	99.96	69.53	2520
HSA-MIR-6780B-5P	99.96	69.60	2562
HSA-MIR-548AJ-3P	99.96	73.38	5345
HSA-MIR-548X-3P	99.96	73.38	5345

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 86.5% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 40)

Jak-Stat and PI 3-kinase activation pathways regulate the TPO-induced survival of megakaryocytic cells via Bcl-xL gene expression. (PMID:11756417)
gene expression level of beta-TUB, Bcl-XL, and GSTpi was closely correlated with the IC50 for docetaxel (PMID:11788897)
regulation of alternative splicing in lung adenocarcinoma cells by de novo ceramide (PMID:11801602)
Bcl-X(L) may regulate Bax translocation through modulation of protein phosphatase or kinase signaling. (PMID:11883953)
Bcl-xL prevents TRAIL-induced apoptosis by abrogating caspase activation and cleavage of BH3 interacting domain death agonist protein in acute myelogenous leukemia HL-60 cells. (PMID:11911810)
Mature dendritic cells are protected from Fas/CD95-mediated apoptosis by upregulation of Bcl-X(L). (PMID:11941452)
Erythrocyte survival is suppressed by a Bak-derived BH3 peptide that interacts with membrane-associated Bcl-X(L). (PMID:11964315)
increased expression associated with low levels of apoptosis in renal cell carcinoma; may have role in progression of cancer and treatment resistance (PMID:12025227)
selective expression of Bcl-xL may be involved in the difference in the susceptibility to cell death between immature dendritic cells and mature dendritic cells . (PMID:12046686)
Antisense strategy shows that Mcl-1 rather than Bcl-2 or Bcl-x(L) is an essential survival protein of human myeloma cells. (PMID:12070027)
In Parkinson’s disease patients, Bcl-xL mRNA expression per dopaminergic neuron is almost double that of controls, an effect that may be mediated by a redistribution of Bcl-xL from the cytosol to the outer mitochondrial membrane. (PMID:12079401)
role in modulating HIV-1/monocyte-derived macrophage-induced neuronal apoptosis (PMID:12186923)
Bcl-XL protects BimEL-induced Bax conformational change and cytochrome C release. (PMID:12198137)
In addition, B cell lymphoma leukemia (Bcl)-x(L), an antiapoptotic regulator, was also highly expressed in macrophages from smokers compared with nonsmokers and subjects with asthma. (PMID:12204872)
overexpression of the Bcl-2 or Bcl-x(L) associated with the loss of apoptosis in breast cancer cells in vivo may account for their metastatic behavior (PMID:12209955)
During endothelial cell apoptosis, Bcl-xl level showed no significant in HUVECs stimulated with TNF-alpha alone or in combination with IFN-gamma. (PMID:12214154)
Data suggest that Bcl-xl has a biochemical function that is capable of partially rescuing loss of function mutations in S. cerevisiae. (PMID:12244097)
Bcl-xL is deamidated in the cellular response to DNA damage and leads to apoptosis resistance (PMID:12372300)
treatment with an antisense oligonucleotide (5’Bcl-x AS) shifts the splicing pattern of Bcl-x pre-mRNA from the anti-apoptotic variant, Bcl-xL, to the pro-apoptotic variant, Bcl-xS (PMID:12381725)
role in inhibiting diamide-induced SM hydrolysis and ceramide accumulation but not the decrease in intracellular GSH (PMID:12387875)
A very low mRNA level was indicated at bax, bcl-2 and bcl-xL in hepatocellular carcinoma tissues in contrast to normal liver. (PMID:12439925)
Mitochondrial targeting of Bcl-x(L) requires the COOH-terminal transmembrane (TM) domain flanked at both ends by at least two basic amino acids (PMID:12515824)
Bcl-xl over-expression does not confer protection against cell death in U937 cells. (PMID:12553012)
BCL-xL levels decreased when H202 was greater than 250 micro M. (PMID:12579342)
findings indicate that the levels of XIAP and Bcl-X(L) are regulated by distinct pathways during monocytic differentiation, and that upregulation of these proteins contributes to the increased longevity of cells in the monocytic lineage (PMID:12592339)
Bcl-x(L) is a key target mediating the anti-apoptotic effects of glucocorticoids during fibrosarcoma development (PMID:12637494)
a novel role in cell fate decisions /during hematopoietic differentiation/ beyond cell survival (PMID:12721288)
Bcl-2 may not play a physiological role in antagonizing apoptosis signals pertinent to BAD activation in prostate cancer cells (PMID:12738789)
Following UV treatment, Mcl-1 protein synthesis is blocked, the existing pool of Mcl-1 protein is rapidly degraded by the proteasome, and cytosolic Bcl-xL translocates to the mitochondria (PMID:12783855)
Human Bcl-xL is deamidated at asparagines 52 and 66 & the rate of deamidation is significantly lower in hepatocellular carcinomas than in normal liver. Tumor cells may gain apoptosis resistance & a survival advantage by suppressing Bcl-xL deamidation. (PMID:12810626)
Bcl-xl has a role in suppressing a p53 and Bax-dependent apoptotic pathway in colorectal cancer cells (PMID:12855666)
Overexpression of bcl-2 and bcl-xL leading to prolonged survival of mast cells may contribute to the pathogenesis of mastocytosis. (PMID:12937123)
bcl-xL directly binds to Apaf-1. (PMID:12963020)
bcl-xL gene overexpression is linked to short overall survival times in follicular lymphoma. (PMID:12969962)
retinoic acid-induced apoptotic signals were transduced via downregulation of Bcl-xL and the decrease in the mitochondrial membrane function leading to caspase-3 activation (PMID:14502257)
Overexpression of bcl-xl is associated with colonic neoplasms (PMID:14520471)
BCL-XL is induced during rapamycin-resistant proliferation of CD8+ T cells (PMID:14573608)
Bcl-XL has a role in preventing Bax activation at the mitochondrial membrane (PMID:14625274)
Bcl-x was associated with increased survival in thymic neoplasms. Bcl-x:Bax ratio was also associated with survival. (PMID:14631373)
Transgenic mice crrossed with c-MYC transgenic mice develop multiple myeloma. (PMID:14656874)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	bcl2l1	ENSDARG00000008434
mus_musculus	Bcl2l1	ENSMUSG00000007659
rattus_norvegicus	AC098008.1	ENSRNOG00000018503

Paralogs (8): BAK1 (ENSG00000030110), BAX (ENSG00000087088), BCL2L2 (ENSG00000129473), BCL2L10 (ENSG00000137875), BCL2A1 (ENSG00000140379), MCL1 (ENSG00000143384), BCL2 (ENSG00000171791), BOK (ENSG00000176720)

Protein

Protein identifiers

Bcl-2-like protein 1 — Q07817 (reviewed: Q07817)

Alternative names: Apoptosis regulator Bcl-X

All UniProt accessions (8): Q07817, A0A0S2Z3C5, A0A7I2V597, Q5QP56, Q5QP59, Q5TE63, Q5TE64, Q9H1R6

UniProt curated annotations — full annotation on UniProt →

Function. Potent inhibitor of cell death. Inhibits activation of caspases. Appears to regulate cell death by blocking the voltage-dependent anion channel (VDAC) by binding to it and preventing the release of the caspase activator, CYC1, from the mitochondrial membrane. Also acts as a regulator of G2 checkpoint and progression to cytokinesis during mitosis. Isoform Bcl-X(L) also regulates presynaptic plasticity, including neurotransmitter release and recovery, number of axonal mitochondria as well as size and number of synaptic vesicle clusters. During synaptic stimulation, increases ATP availability from mitochondria through regulation of mitochondrial membrane ATP synthase F(1)F(0) activity and regulates endocytic vesicle retrieval in hippocampal neurons through association with DMN1L and stimulation of its GTPase activity in synaptic vesicles. May attenuate inflammation impairing NLRP1-inflammasome activation, hence CASP1 activation and IL1B release. Isoform Bcl-X(S) promotes apoptosis.

Subunit / interactions. Homodimer. Interacts with BCL2L11. Interacts with BAD. Interacts with PGAM5. Interacts with HEBP2. Interacts with p53/TP53 and BBC3; interaction with BBC3 disrupts the interaction with p53/TP53. Interacts with ATP5F1A and ATP5F1B; the interactions mediate the association of isoform Bcl-X(L) with the mitochondrial membrane ATP synthase F(1)F(0) ATP synthase. Interacts with VDAC1. Interacts with BCL2L11 (via BH3). Interacts with RNF183. Interacts with GIMAP3/IAN4 and GIMAP5/IAN5. Interacts with GIMAP5 and HSPA8/HSC70; the interaction between HSPA8 and BCL2L1 is impaired in the absence of GIMAP5. Interacts with isoform 4 of CLU; this interaction releases and activates BAX and promotes cell death. Forms heterodimers with BAX, BAK or BCL2; heterodimerization with BAX does not seem to be required for anti-apoptotic activity. Interacts with isoform 1 of SIVA1; the interaction inhibits the anti-apoptotic activity. Interacts with IKZF3. Interacts with RTL10/BOP. Interacts with DNM1L and CLTA; DNM1L and BCL2L1 isoform BCL-X(L) may form a complex in synaptic vesicles that also contains clathrin and MFF. Interacts (via the loop between motifs BH4 and BH3) with NLRP1 (via LRR repeats), but not with NLRP2, NLRP3, NLRP4, PYCARD, nor MEFV. Interacts with BECN1.

Subcellular location. Mitochondrion inner membrane. Mitochondrion outer membrane. Mitochondrion matrix. Cytoplasmic vesicle. Secretory vesicle. Synaptic vesicle membrane. Cytoplasm. Cytosol. Cytoskeleton. Microtubule organizing center. Centrosome. Nucleus membrane.

Tissue specificity. Bcl-X(S) is expressed at high levels in cells that undergo a high rate of turnover, such as developing lymphocytes. In contrast, Bcl-X(L) is found in tissues containing long-lived postmitotic cells, such as adult brain.

Post-translational modifications. Proteolytically cleaved by caspases during apoptosis. The cleaved protein, lacking the BH4 motif, has pro-apoptotic activity. Phosphorylated on Ser-62 by CDK1. This phosphorylation is partial in normal mitotic cells, but complete in G2-arrested cells upon DNA-damage, thus promoting subsequent apoptosis probably by triggering caspases-mediated proteolysis. Phosphorylated by PLK3, leading to regulate the G2 checkpoint and progression to cytokinesis during mitosis. Phosphorylation at Ser-49 appears during the S phase and G2, disappears rapidly in early mitosis during prometaphase, metaphase and early anaphase, and re-appears during telophase and cytokinesis. Ubiquitinated by RNF183 during prolonged ER stress, leading to degradation by the proteosome.

Domain organisation. The BH4 motif is required for anti-apoptotic activity. The BH1 and BH2 motifs are required for both heterodimerization with other Bcl-2 family members and for repression of cell death. The loop between motifs BH4 and BH3 is required for the interaction with NLRP1.

Similarity. Belongs to the Bcl-2 family.

Isoforms (3)

UniProt ID	Names	Canonical?
Q07817-1	Bcl-X(L), Bcl-xL	yes
Q07817-2	Bcl-X(S), Bcl-xS
Q07817-3	Bcl-X(beta)

RefSeq proteins (10): NP_001182, NP_001304848, NP_001304849, NP_001304850, NP_001309168, NP_001309169, NP_001309171, NP_001411260, NP_001411261, NP_612815* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002475	Bcl2-like	Family
IPR003093	Bcl2_BH4	Domain
IPR004725	Bcl2/BclX	Family
IPR013279	Apop_reg_BclX	Family
IPR020717	Bcl2_BH1_motif_CS	Conserved_site
IPR020726	Bcl2_BH2_motif_CS	Conserved_site
IPR020728	Bcl2_BH3_motif_CS	Conserved_site
IPR020731	Bcl2_BH4_motif_CS	Conserved_site
IPR026298	Bcl-2_fam	Family
IPR036834	Bcl-2-like_sf	Homologous_superfamily
IPR046371	Bcl-2_BH1-3	Domain

Pfam: PF00452, PF02180

UniProt features (52 total): helix 14, mutagenesis site 13, turn 6, strand 5, short sequence motif 4, splice variant 2, sequence conflict 2, modified residue 2, chain 1, transmembrane region 1, region of interest 1, site 1

Structure

Experimental structures (PDB)

118 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
7JGW	X-RAY DIFFRACTION	1.3
3SP7	X-RAY DIFFRACTION	1.4
7YAA	X-RAY DIFFRACTION	1.4
7LH7	X-RAY DIFFRACTION	1.41
4QVF	X-RAY DIFFRACTION	1.53
4A1U	X-RAY DIFFRACTION	1.54
6VWC	X-RAY DIFFRACTION	1.6
6O0K	X-RAY DIFFRACTION	1.62
3SPF	X-RAY DIFFRACTION	1.7
9O14	X-RAY DIFFRACTION	1.73
9O16	X-RAY DIFFRACTION	1.73
5FMK	X-RAY DIFFRACTION	1.73
6O0M	X-RAY DIFFRACTION	1.75
4BPK	X-RAY DIFFRACTION	1.76
8VWX	X-RAY DIFFRACTION	1.77
3FDL	X-RAY DIFFRACTION	1.78
6ST2	X-RAY DIFFRACTION	1.79
2YQ6	X-RAY DIFFRACTION	1.8
4TUH	X-RAY DIFFRACTION	1.8
6O0P	X-RAY DIFFRACTION	1.8
5VAY	X-RAY DIFFRACTION	1.8
6UVC	X-RAY DIFFRACTION	1.9
6YLI	X-RAY DIFFRACTION	1.9
7XGF	X-RAY DIFFRACTION	1.9
7XGG	X-RAY DIFFRACTION	1.9
2YQ7	X-RAY DIFFRACTION	1.9
6ZHC	X-RAY DIFFRACTION	1.92
5VX3	X-RAY DIFFRACTION	1.95
1R2D	X-RAY DIFFRACTION	1.95
3R85	X-RAY DIFFRACTION	1.95

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q07817-F1	73.34	0.39

Functional residue map

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

Catalytic / active sites (1): 61–62 (cleavage; by caspase-1)

Post-translational modifications (2): 49, 62

Mutagenesis-validated functional residues (13):

Position	Phenotype
49	less stable at g2 checkpoint after dna damage.
61	no cleavage by caspase-1 nor by caspase-3.
131–133	no heterodimerization with bax.
135–137	loss of anti-apoptotic activity.
138–140	loss of anti-apoptotic activity.
138	no heterodimerization with bax.
145–147	decreases interaction with dnm1l, no effect on endocytosis enhancement.
148	no heterodimerization with bax.
156	no effect on caspase-1 cleavage.
176	no effect on caspase-1 cleavage.
188–191	abolishes interaction with dnm1l and endocytosis enhancement.
188–189	reduces anti-apoptotic activity by about half.
189	no effect on caspase-1 cleavage.

Function

Pathways and Gene Ontology

Reactome pathways

34 pathways

ID	Pathway
R-HSA-111453	BH3-only proteins associate with and inactivate anti-apoptotic BCL-2 members
R-HSA-6785807	Interleukin-4 and Interleukin-13 signaling
R-HSA-844455	The NLRP1 inflammasome
R-HSA-9648002	RAS processing
R-HSA-9692913	SARS-CoV-1-mediated effects on programmed cell death
R-HSA-9702518	STAT5 activation downstream of FLT3 ITD mutants
R-HSA-9818030	NFE2L2 regulating tumorigenic genes
R-HSA-109581	Apoptosis
R-HSA-109606	Intrinsic Pathway for Apoptosis
R-HSA-1280215	Cytokine Signaling in Immune system
R-HSA-162582	Signal Transduction
R-HSA-1643685	Disease
R-HSA-168249	Innate Immune System
R-HSA-168256	Immune System
R-HSA-168643	Nucleotide-binding domain, leucine rich repeat containing receptor (NLR) signaling pathways
R-HSA-2262752	Cellular responses to stress
R-HSA-449147	Signaling by Interleukins
R-HSA-5357801	Programmed Cell Death
R-HSA-5663202	Diseases of signal transduction by growth factor receptors and second messengers
R-HSA-5663205	Infectious disease
R-HSA-5673001	RAF/MAP kinase cascade
R-HSA-5683057	MAPK family signaling cascades
R-HSA-5684996	MAPK1/MAPK3 signaling
R-HSA-622312	Inflammasomes
R-HSA-8953897	Cellular responses to stimuli
R-HSA-9678108	SARS-CoV-1 Infection
R-HSA-9679506	SARS-CoV Infections
R-HSA-9682385	FLT3 signaling in disease
R-HSA-9692914	SARS-CoV-1-host interactions
R-HSA-9703648	Signaling by FLT3 ITD and TKD mutants

MSigDB gene sets: 578 (showing top): GOBP_NEGATIVE_REGULATION_OF_RESPONSE_TO_ENDOPLASMIC_RETICULUM_STRESS, GGGACCA_MIR133A_MIR133B, MYAATNNNNNNNGGC_UNKNOWN, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_NEGATIVE_REGULATION_OF_NEURON_APOPTOTIC_PROCESS, RODRIGUES_THYROID_CARCINOMA_ANAPLASTIC_UP, GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, GOBP_RESPONSE_TO_IONIZING_RADIATION, GOBP_REGULATION_OF_AUTOPHAGY, WANG_CLIM2_TARGETS_UP, BUYTAERT_PHOTODYNAMIC_THERAPY_STRESS_DN, REACTOME_INNATE_IMMUNE_SYSTEM, BOYLAN_MULTIPLE_MYELOMA_PCA1_DN, GCM_GSPT1, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM

GO Biological Process (56): ovarian follicle development (GO:0001541), in utero embryonic development (GO:0001701), release of cytochrome c from mitochondria (GO:0001836), endocytosis (GO:0006897), germ cell development (GO:0007281), spermatogenesis (GO:0007283), male gonad development (GO:0008584), intrinsic apoptotic signaling pathway in response to DNA damage (GO:0008630), apoptotic mitochondrial changes (GO:0008637), fertilization (GO:0009566), negative regulation of autophagy (GO:0010507), regulation of cytokinesis (GO:0032465), positive regulation of mononuclear cell proliferation (GO:0032946), response to cytokine (GO:0034097), ectopic germ cell programmed cell death (GO:0035234), regulation of growth (GO:0040008), positive regulation of apoptotic process (GO:0043065), negative regulation of apoptotic process (GO:0043066), negative regulation of neuron apoptotic process (GO:0043524), dendritic cell proliferation (GO:0044565), response to cycloheximide (GO:0046898), regulation of mitochondrial membrane permeability (GO:0046902), epithelial cell proliferation (GO:0050673), negative regulation of developmental process (GO:0051093), neuron apoptotic process (GO:0051402), defense response to virus (GO:0051607), regulation of mitochondrial membrane potential (GO:0051881), cellular response to amino acid stimulus (GO:0071230), cellular response to alkaloid (GO:0071312), cellular response to gamma radiation (GO:0071480), apoptotic process in bone marrow cell (GO:0071839), negative regulation of release of cytochrome c from mitochondria (GO:0090201), dendritic cell apoptotic process (GO:0097048), extrinsic apoptotic signaling pathway in absence of ligand (GO:0097192), hepatocyte apoptotic process (GO:0097284), negative regulation of execution phase of apoptosis (GO:1900118), negative regulation of mitochondrial outer membrane permeabilization involved in apoptotic signaling pathway (GO:1901029), negative regulation of extrinsic apoptotic signaling pathway via death domain receptors (GO:1902042), negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage (GO:1902230), negative regulation of endoplasmic reticulum stress-induced intrinsic apoptotic signaling pathway (GO:1902236)

GO Molecular Function (5): channel activity (GO:0015267), protein kinase binding (GO:0019901), identical protein binding (GO:0042802), BH3 domain binding (GO:0051434), protein binding (GO:0005515)

GO Cellular Component (17): cytoplasm (GO:0005737), mitochondrion (GO:0005739), mitochondrial outer membrane (GO:0005741), mitochondrial inner membrane (GO:0005743), mitochondrial matrix (GO:0005759), endoplasmic reticulum (GO:0005783), centrosome (GO:0005813), cytosol (GO:0005829), synaptic vesicle membrane (GO:0030672), nuclear membrane (GO:0031965), Bcl-2 family protein complex (GO:0097136), nucleus (GO:0005634), cytoskeleton (GO:0005856), membrane (GO:0016020), cytoplasmic vesicle (GO:0031410), mitochondrial membrane (GO:0031966), synapse (GO:0045202)

Reactome top-level categories

Rollup of top-14 pathways:

Category	Pathways
Immune System	2
Disease	2
Intrinsic Pathway for Apoptosis	1
Signaling by Interleukins	1
Inflammasomes	1
RAF/MAP kinase cascade	1
SARS-CoV-1-host interactions	1
Signaling by FLT3 ITD and TKD mutants	1
Nuclear events mediated by NFE2L2	1
Programmed Cell Death	1
Apoptosis	1
Innate Immune System	1
Cellular responses to stimuli	1
Cytokine Signaling in Immune system	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cytoplasm	4
developmental process involved in reproduction	3
apoptotic process	3
cellular anatomical structure	3
intracellular membrane-bounded organelle	3
mononuclear cell proliferation	2
regulation of apoptotic process	2
mitochondrial membrane	2
mitochondrion	2
organelle membrane	2
female gonad development	1
anatomical structure development	1
chordate embryonic development	1
apoptotic mitochondrial changes	1
apoptotic signaling pathway	1
vesicle budding from membrane	1
membrane invagination	1
vesicle-mediated transport	1
import into cell	1
gamete generation	1
cellular process involved in reproduction in multicellular organism	1
cell development	1
male gamete generation	1
gonad development	1
development of primary male sexual characteristics	1
DNA damage response	1
intrinsic apoptotic signaling pathway	1
mitochondrion organization	1
sexual reproduction	1
reproductive process	1
autophagy	1
negative regulation of catabolic process	1
regulation of autophagy	1
cytokinesis	1
regulation of cell cycle process	1
regulation of cell division	1
regulation of mononuclear cell proliferation	1
positive regulation of leukocyte proliferation	1
response to peptide	1
programmed cell death involved in cell development	1

Protein interactions and networks

STRING

5006 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
BCL2L1	BCL2L11	O43521	999
BCL2L1	TP53	P04637	998
BCL2L1	PMAIP1	Q13794	998
BCL2L1	HRK	O00198	997
BCL2L1	BECN1	Q14457	996
BCL2L1	VDAC1	P21796	995
BCL2L1	APAF1	O14727	992
BCL2L1	ATG5	Q9H1Y0	990
BCL2L1	BBC3	Q96PG8	988
BCL2L1	BIK	Q13323	987
BCL2L1	BMF	Q96LC9	986
BCL2L1	BCL2	P10415	984
BCL2L1	BNIP3	Q12983	983
BCL2L1	NLRP1	Q9C000	974
BCL2L1	RTL10	Q7L3V2	972

IntAct

281 interactions, top by confidence:

A	B	Type	Score
BCL2L1	BAD	psi-mi:“MI:0915”(physical association)	0.980
BAD	BCL2L1	psi-mi:“MI:0915”(physical association)	0.980
BAD	BCL2L1	psi-mi:“MI:2364”(proximity)	0.980
BCL2L1	BAD	psi-mi:“MI:2364”(proximity)	0.980

BioGRID (460): BCL2L11 (Protein-peptide), BID (Protein-peptide), BAD (Protein-peptide), BIK (Protein-peptide), BMF (Protein-peptide), HRK (Protein-peptide), PMAIP1 (Protein-peptide), BBC3 (Protein-peptide), BCL2L1 (Reconstituted Complex), BCL2L1 (Affinity Capture-Western), TP53BP2 (Protein-peptide), TP53BP2 (Co-crystal Structure), BCL2L1 (Reconstituted Complex), TPT1 (Reconstituted Complex), TPT1 (Affinity Capture-Western)

ESM2 similar proteins: A3KN95, A4IFG4, A4IG66, A7E2I7, A7S641, O77737, P53563, Q07817, Q0IHF1, Q0VCF5, Q17QW2, Q23387, Q2M146, Q3C2P8, Q4QQM5, Q5BLE2, Q5RDN2, Q5U2V9, Q5XJS0, Q5Y171, Q5YLM1, Q5ZLD4, Q626N3, Q66H44, Q68EF0, Q68FE7, Q6DF19, Q6GL42, Q6GQT5, Q6GR21, Q6NRB7, Q6NRI4, Q6NYK3, Q6WQJ1, Q6ZPQ6, Q7Z698, Q810L4, Q8BG50, Q8IW70, Q8N4L1

Diamond homologs: O02703, O02718, O77737, P10415, P10417, P49950, P53563, P70345, Q00709, Q07812, Q07813, Q07816, Q07817, Q07820, Q1RMX3, Q45T69, Q63690, Q64373, Q6R755, Q7YRZ9, Q90343, Q91827, Q92843, Q9JJV8, O08734, Q07440, Q07818, Q16548, Q16611, Q3C2I0, Q91828, P0C8H4, P0C8H5, P0C8H6, P42485, Q07819, Q90ZN1, Q9HBF5, Q8HYS5, P97287

SIGNOR signaling

46 interactions.

A	Effect	B	Mechanism
chelerythrine	down-regulates	BCL2L1	“chemical inhibition”
BAD	“down-regulates activity”	BCL2L1	binding
BBC3	“down-regulates activity”	BCL2L1	binding
BCL2L11	down-regulates	BCL2L1	binding
CREB1	“up-regulates quantity by expression”	BCL2L1	“transcriptional regulation”
ABT-737	down-regulates	BCL2L1	“chemical inhibition”
BCL2L1	down-regulates	BAK1	binding
BCL2L1	down-regulates	BECN1	binding
PLK3	up-regulates	BCL2L1	phosphorylation
SH2B3	“down-regulates quantity by repression”	BCL2L1	“transcriptional regulation”
BCL2L11	“down-regulates activity”	BCL2L1	binding
4-[4-[[2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohexenyl]methyl]-1-piperazinyl]-N-[4-[[(2R)-4-(4-morpholinyl)-1-(phenylthio)butan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide	down-regulates	BCL2L1	“chemical inhibition”
N-[4-(2-tert-butylphenyl)sulfonylphenyl]-2,3,4-trihydroxy-5-[(2-propan-2-ylphenyl)methyl]benzamide	down-regulates	BCL2L1	“chemical inhibition”
BID	“down-regulates activity”	BCL2L1	binding
EIF3E	“up-regulates quantity”	BCL2L1	“translation regulation”
E	“down-regulates activity”	BCL2L1
7a	“down-regulates activity”	BCL2L1	binding
LGALS3	“up-regulates quantity by stabilization”	BCL2L1
BIK	down-regulates	BCL2L1	binding
CDK1	“down-regulates activity”	BCL2L1	phosphorylation
hsa-miR-491-5p	“down-regulates quantity by repression”	BCL2L1	“post transcriptional regulation”
CDK2	“up-regulates activity”	BCL2L1	phosphorylation
RNF183	“down-regulates quantity by destabilization”	BCL2L1	ubiquitination
PRKN	“down-regulates quantity by destabilization”	BCL2L1	ubiquitination
IKBKB	“down-regulates quantity”	BCL2L1	phosphorylation
HRK	down-regulates	BCL2L1	binding
BCL2L1	“down-regulates activity”	APAF1	binding
BCL2L1	“down-regulates activity”	CASP9	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 46 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
Activation of BH3-only proteins	6	114.6×	5e-10
Intrinsic Pathway for Apoptosis	7	78.8×	2e-10
Apoptosis	7	45.2×	6e-09
Programmed Cell Death	7	39.4×	1e-08

GO biological processes:

GO term	Partners	Fold	FDR
positive regulation of release of cytochrome c from mitochondria	8	170.2×	3e-14
release of cytochrome c from mitochondria	5	97.5×	2e-07
positive regulation of protein-containing complex assembly	7	65.5×	2e-09
intrinsic apoptotic signaling pathway	5	49.8×	6e-06
positive regulation of apoptotic process	8	12.6×	2e-05

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	11
Likely benign	3
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

907 predictions. Top by Δscore:

Variant	Effect	Δscore
20:31666082:GTATC:G	acceptor_gain	1.0000
20:31666083:TATC:T	acceptor_gain	1.0000
20:31666084:ATC:A	acceptor_gain	1.0000
20:31666085:TC:T	acceptor_gain	1.0000
20:31666086:CC:C	acceptor_gain	1.0000
20:31666087:C:CC	acceptor_gain	1.0000
20:31666087:CTGCA:C	acceptor_loss	1.0000
20:31666088:T:A	acceptor_loss	1.0000
20:31666087:C:T	acceptor_gain	0.9900
20:31666090:C:CT	acceptor_gain	0.9900
20:31720332:T:A	donor_gain	0.9900
20:31721653:A:AC	donor_gain	0.9800
20:31721654:C:CC	donor_gain	0.9800
20:31721654:CCCAG:C	donor_gain	0.9800
20:31666091:A:T	acceptor_gain	0.9700
20:31721653:AC:A	donor_gain	0.9700
20:31721654:CC:C	donor_gain	0.9700
20:31720514:G:A	donor_gain	0.9600
20:31721649:TCTTA:T	donor_loss	0.9600
20:31721650:CT:C	donor_loss	0.9600
20:31721651:TTAC:T	donor_loss	0.9600
20:31721652:T:TC	donor_loss	0.9600
20:31721653:A:G	donor_loss	0.9600
20:31721654:C:A	donor_loss	0.9600
20:31689343:CA:C	donor_gain	0.9400
20:31670448:T:A	donor_gain	0.9300
20:31689324:ATG:A	donor_gain	0.9300
20:31721647:GTTCT:G	donor_loss	0.9200
20:31721648:TTCTT:T	donor_loss	0.9200
20:31666968:A:C	donor_gain	0.9100

AlphaMissense

1542 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
20:31721655:C:A	W188C	1.000
20:31721655:C:G	W188C	1.000
20:31721657:A:G	W188R	1.000
20:31721657:A:T	W188R	1.000
20:31721779:C:T	G147D	1.000
20:31721781:G:C	F146L	1.000
20:31721781:G:T	F146L	1.000
20:31721783:A:G	F146L	1.000
20:31721794:G:T	A142D	1.000
20:31721803:C:G	R139P	1.000
20:31721806:C:T	G138D	1.000
20:31721807:C:G	G138R	1.000
20:31721808:C:A	W137C	1.000
20:31721808:C:G	W137C	1.000
20:31721810:A:G	W137R	1.000
20:31721810:A:T	W137R	1.000
20:31721826:G:C	F131L	1.000
20:31721826:G:T	F131L	1.000
20:31721828:A:G	F131L	1.000
20:31721850:A:C	F123L	1.000
20:31721850:A:T	F123L	1.000
20:31721852:A:G	F123L	1.000
20:31721904:G:C	F105L	1.000
20:31721904:G:T	F105L	1.000
20:31721906:A:G	F105L	1.000
20:31665986:C:T	G222D	0.999
20:31665987:C:G	G222R	0.999
20:31665989:G:T	A221D	0.999
20:31666079:A:G	F191S	0.999
20:31721656:C:G	W188S	0.999

dbSNP variants (sampled 300 via entrez): RS1000004123 (20:31694052 G>C), RS1000022353 (20:31697807 C>T), RS1000033843 (20:31697517 A>C,G), RS1000168398 (20:31692863 C>G,T), RS1000213621 (20:31687344 T>C), RS1000240519 (20:31670134 T>C), RS1000265766 (20:31679990 A>G,T), RS1000281201 (20:31690994 TA>T,TAA), RS1000293006 (20:31669835 A>C), RS1000299758 (20:31684579 A>G,T), RS1000301782 (20:31725743 G>A), RS1000317680 (20:31680383 C>G,T), RS1000343264 (20:31701139 C>T), RS1000404432 (20:31695766 G>T), RS1000442620 (20:31677105 T>C)

Disease associations

OMIM: gene MIM:600039 | disease phenotypes:

GenCC curated gene-disease

Mondo (1): hereditary breast ovarian cancer syndrome (MONDO:0003582)

Orphanet (1): Hereditary breast and/or ovarian cancer syndrome (Orphanet:145)

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

15 associations (top):

Study	Trait	p-value
GCST002756_3	Subcortical brain region volumes	1.000000e-12
GCST003030_10	Oppositional defiant disorder dimensions in attention-deficit hyperactivity disorder	3.000000e-06
GCST003030_9	Oppositional defiant disorder dimensions in attention-deficit hyperactivity disorder	4.000000e-06
GCST004603_281	Platelet count	3.000000e-24
GCST004607_32	Plateletcrit	4.000000e-32
GCST004609_156	Monocyte percentage of white cells	2.000000e-11
GCST004639_6	Prudent dietary pattern	2.000000e-06
GCST005083_10	Putamen volume	2.000000e-09
GCST009067_1	Mosaic loss of chromosome Y (Y chromosome dosage)	2.000000e-17
GCST010703_295	Brain morphology (MOSTest)	1.000000e-14
GCST90002381_359	Eosinophil count	1.000000e-30
GCST90002382_528	Eosinophil percentage of white cells	1.000000e-27
GCST90002393_331	Monocyte count	1.000000e-12
GCST90002400_294	Plateletcrit	1.000000e-63
GCST90002402_586	Platelet count	1.000000e-50

EFO canonical traits (10, from GWAS)

EFO ID	Trait name
EFO:0007679	oppositional defiant disorder measurement
EFO:0004309	platelet count
EFO:0007985	platelet crit
EFO:0007989	monocyte percentage of leukocytes
EFO:0008111	diet measurement
EFO:0007783	mosaic loss of chromosome Y measurement
EFO:0004346	neuroimaging measurement
EFO:0004842	eosinophil count
EFO:0007991	eosinophil percentage of leukocytes
EFO:0005091	monocyte count

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
D061325	Hereditary Breast and Ovarian Cancer Syndrome	C04.588.180.483; C04.588.322.455.431; C04.700.517; C12.050.351.500.056.630.705.431; C12.050.351.937.418.685.431; C12.100.250.056.630.705.431; C12.900.418.685.431; C16.320.700.517; C17.800.090.500.483; C19.344.410.431; C19.391.630.705.431

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (10): CHEMBL3137283 (PROTEIN-PROTEIN INTERACTION), CHEMBL3883285 (PROTEIN-PROTEIN INTERACTION), CHEMBL3883286 (PROTEIN-PROTEIN INTERACTION), CHEMBL3883287 (PROTEIN-PROTEIN INTERACTION), CHEMBL3883288 (PROTEIN-PROTEIN INTERACTION), CHEMBL4523705 (PROTEIN-PROTEIN INTERACTION), CHEMBL4625 (SINGLE PROTEIN), CHEMBL4748229 (PROTEIN-PROTEIN INTERACTION), CHEMBL5169267 (PROTEIN-PROTEIN INTERACTION), CHEMBL6177906 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

13 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 61,185 (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
CHEMBL1200938	METHYSERGIDE MALEATE	4	4
CHEMBL3137309	VENETOCLAX	4	9,389
CHEMBL297453	EPIGALOCATECHIN GALLATE	3	22,804
CHEMBL51483	GOSSYPOL	3	13,973
CHEMBL443684	NAVITOCLAX	3	4,791
CHEMBL2107358	OBATOCLAX MESYLATE	3	471
CHEMBL408194	OBATOCLAX	3	2,914
CHEMBL5314951	SONROTOCLAX	3	3
CHEMBL5754780	ASARETOCLAX	2	14
CHEMBL376408	ABT 737	1	4,288
CHEMBL4297482	AZD-5991	1	947
CHEMBL4446378	TAPOTOCLAX	1	1,476
CHEMBL4745523	DT-2216	1	111

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: other protein — B-cell lymphoma 2 (Bcl-2) protein family

Most potent curated ligand interactions (8 total), top 8:

Ligand	Action	Affinity	Parameter
APG-1252-M1	Antagonist	9.87	pKi
lisaftoclax	Antagonist	9.3	pKi
ABT-737	Antagonist	9.3	pKi
AZD4320	Antagonist	9.0	pIC50
navitoclax	Antagonist	9.0	pKi
A-1331852	Antagonist	8.2	pEC50
venetoclax	Antagonist	7.32	pKi
obatoclax	Antagonist	5.33	pKi

Binding affinities (BindingDB)

947 measured of 1055 human assays (1075 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-2-[(6,7-difluoro-1H-indol-5-yl)oxy]-N-[(5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)sulfonyl]benzamide	KI	0.039 nM	US-9493431: Apoptosis-inducing agent for the treatment of cancer and immune and autoimmune diseases
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonyl-1,3-thiazole-4-carboxamide	KI	0.04 nM	US-8883784: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[(5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)sulfonyl]-2-[(6-fluoro-1H-indol-5-yl)oxy]benzamide	KI	0.053 nM	US-9493431: Apoptosis-inducing agent for the treatment of cancer and immune and autoimmune diseases
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-N-[4-[3-(dimethylamino)propylamino]-3-(trifluoromethylsulfonyl)phenyl]sulfonyl-5-(2-phenylethyl)-1,3-thiazole-4-carboxamide	KI	0.06 nM	US-8883784: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
4-[4-[[2-(4-chlorophenyl)cyclohexen-1-yl]methyl]piperazin-1-yl]-N-[5-[[(2R)-4-[methyl(propan-2-yl)amino]-1-phenylsulfanylbutan-2-yl]amino]-4-nitrothiophen-2-yl]sulfonylbenzamide	KI	0.064 nM	US-9493431: Apoptosis-inducing agent for the treatment of cancer and immune and autoimmune diseases
4-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[5-[[(2R)-4-[methyl(propan-2-yl)amino]-1-phenylsulfanylbutan-2-yl]amino]-4-nitrothiophen-2-yl]sulfonylbenzamide	KI	0.084 nM	US-9493431: Apoptosis-inducing agent for the treatment of cancer and immune and autoimmune diseases
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-1,3-thiazole-4-carboxamide	KI	0.1 nM	US-8883784: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonyl-1,3-thiazole-4-carboxamide	KI	0.1 nM	US-8883784: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-(3-benzylphenyl)pyridine-2-carboxylic acid	KI	0.1 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[3-(3,3-dimethylcyclohexyl)oxy-2-methylphenyl]pyridine-2-carboxylic acid	KI	0.1 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-1,3-thiazole-4-carboxamide	KI	0.14 nM	US-8883784: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-N-[4-[[(2R)-4-hydroxy-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonyl-1,3-thiazole-4-carboxamide	KI	0.2 nM	US-8883784: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[3-(cyclohexylmethyl)-2-methylphenyl]pyridine-2-carboxylic acid	KI	0.2 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-(3-cyclohexyloxy-2-methylphenyl)pyridine-2-carboxylic acid	KI	0.2 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[3-(cyclohexylamino)-2-methylphenyl]pyridine-2-carboxylic acid	KI	0.2 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[1-[[(1R,2R,5S)-2-(2-methoxyethyl)-6,6-dimethyl-3-bicyclo[3.1.1]heptanyl]methyl]pyrazol-4-yl]pyridine-2-carboxylic acid	KI	0.2 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[2-methyl-3-(N-methylanilino)phenyl]pyridine-2-carboxylic acid	KI	0.2 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[3-[(3,3-dimethylcyclohexyl)methylamino]-2-methylphenyl]pyridine-2-carboxylic acid	KI	0.2 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
3-[3-[2-(1-adamantyl)pyrrolidin-1-yl]-2-cyanophenyl]-6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]pyridine-2-carboxylic acid	KI	0.2 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
4-[4-[(R)-[2-(4-chlorophenyl)phenyl]-hydroxymethyl]piperidin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide	IC50	0.3 nM	US-9018381: Chemical compounds
4-[4-[(R)-[2-(4-chlorophenyl)phenyl]-hydroxymethyl]piperidin-1-yl]-N-[4-[[(2R)-4-[(3S)-3-(diethylaminomethyl)morpholin-4-yl]-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide	IC50	0.3 nM	US-9018381: Chemical compounds
4-[4-[(R)-[2-(4-chlorophenyl)phenyl]-hydroxymethyl]piperidin-1-yl]-N-[4-[[(2R)-4-[(3R)-3-(diethylaminomethyl)morpholin-4-yl]-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide	IC50	0.3 nM	US-9018381: Chemical compounds
4-[4-[(R)-[2-(4-chlorophenyl)phenyl]-hydroxymethyl]piperidin-1-yl]-N-[4-[[(2R)-4-[(3S)-3-[(dimethylamino)methyl]morpholin-4-yl]-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide	IC50	0.3 nM	US-9248140: Chemical compounds
4-[4-[(R)-[2-(4-chlorophenyl)phenyl]-hydroxymethyl]piperidin-1-yl]-N-[4-[[(2R)-4-[(3R)-3-(ethylaminomethyl)morpholin-4-yl]-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide	IC50	0.3 nM	US-9248140: Chemical compounds
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-(2-methyl-3-phenoxyphenyl)pyridine-2-carboxylic acid	KI	0.3 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-(1-benzylpyrrol-3-yl)pyridine-2-carboxylic acid	KI	0.3 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[1-(oxan-2-ylmethyl)pyrazol-4-yl]pyridine-2-carboxylic acid	KI	0.3 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-(1-benzylindazol-5-yl)pyridine-2-carboxylic acid	KI	0.3 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
4-[4-[[2-(4-chlorophenyl)-5,5-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[5-[[(2R)-4-[methyl(propan-2-yl)amino]-1-phenylsulfanylbutan-2-yl]amino]-4-nitrothiophen-2-yl]sulfonylbenzamide	KI	0.307 nM	US-9493431: Apoptosis-inducing agent for the treatment of cancer and immune and autoimmune diseases
4-[4-[(R)-[2-(4-chlorophenyl)phenyl]-hydroxymethyl]piperidin-1-yl]-N-[4-[[(2R)-4-[(3R)-3-(hydroxymethyl)morpholin-4-yl]-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide	IC50	0.4 nM	US-9018381: Chemical compounds
4-[4-[(R)-[2-(4-chlorophenyl)phenyl]-hydroxymethyl]piperidin-1-yl]-N-[4-[[(2R)-4-[(3S)-3-(hydroxymethyl)morpholin-4-yl]-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide	IC50	0.4 nM	US-9018381: Chemical compounds
4-[4-[(R)-[2-(4-chlorophenyl)phenyl]-hydroxymethyl]piperidin-1-yl]-N-[4-[[(2R)-4-[2-(diethylaminomethyl)morpholin-4-yl]-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide	IC50	0.4 nM	US-9018381: Chemical compounds
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[1-[[1-(2-methoxyethoxy)cyclohexyl]methyl]-5-methylpyrazol-4-yl]pyridine-2-carboxylic acid	KI	0.4 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[3-cyclohexyloxy-2-(trifluoromethyl)phenyl]pyridine-2-carboxylic acid	KI	0.4 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-(2-cyclohexyloxy-4-pyridinyl)pyridine-2-carboxylic acid	KI	0.4 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-1-methyl-3,4-dihydro-1H-isoquinolin-2-yl]-3-[5-methyl-1-[(1-methylcyclohexyl)methyl]pyrazol-4-yl]pyridine-2-carboxylic acid	KI	0.4 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-(1-benzylindazol-4-yl)pyridine-2-carboxylic acid	KI	0.4 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
2-(3-chlorophenoxy)-4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[(5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)sulfonyl]benzamide	KI	0.407 nM	US-9493431: Apoptosis-inducing agent for the treatment of cancer and immune and autoimmune diseases
4-[4-[(R)-[2-(4-chlorophenyl)phenyl]-hydroxymethyl]piperidin-1-yl]-N-[4-[[(2R)-4-[ethyl(2-hydroxyethyl)amino]-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide	IC50	0.5 nM	US-9018381: Chemical compounds
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[5-methyl-1-[[2-(2-morpholin-4-ylethoxy)phenyl]methyl]pyrazol-4-yl]pyridine-2-carboxylic acid	KI	0.5 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[5-methyl-1-[(1-methylcyclohexyl)methyl]pyrazol-4-yl]pyridine-2-carboxylic acid	KI	0.5 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[1-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]pyrazol-4-yl]pyridine-2-carboxylic acid	KI	0.5 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[1-[[2-(2-methoxyethoxy)phenyl]methyl]-5-methylpyrazol-4-yl]pyridine-2-carboxylic acid	KI	0.5 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-(3-methyl-2-phenoxy-4-pyridinyl)pyridine-2-carboxylic acid	KI	0.5 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-(1-benzylpyrrolo[2,3-c]pyridin-3-yl)pyridine-2-carboxylic acid	KI	0.5 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
4-[4-[(R)-[2-(4-chlorophenyl)phenyl]-hydroxymethyl]piperidin-1-yl]-N-[4-[[(2R)-4-[(2R)-2-(hydroxymethyl)morpholin-4-yl]-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide	IC50	0.6 nM	US-9018381: Chemical compounds
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[1-[[2-[2-(dimethylamino)ethoxy]phenyl]methyl]-5-methylpyrazol-4-yl]pyridine-2-carboxylic acid	KI	0.6 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[5-methyl-1-[[2-(3-morpholin-4-ylpropoxy)phenyl]methyl]pyrazol-4-yl]pyridine-2-carboxylic acid	KI	0.6 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-(3-phenoxyphenyl)pyridine-2-carboxylic acid	KI	0.6 nM	US-9266877: Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
US20250179047, Example 198	KI	0.6 nM	US-20250179047

ChEMBL bioactivities

2201 potent at pChembl≥5 of 2491 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	Ki	0.01	nM	CHEMBL3342333
10.82	Ki	0.015	nM	CHEMBL6152140
10.74	Ki	0.018	nM	CHEMBL6151196
10.70	Ki	0.02	nM	CHEMBL3342197
10.70	Ki	0.02	nM	CHEMBL6146635
10.57	Ki	0.027	nM	CHEMBL3935328
10.52	Ki	0.03	nM	CHEMBL3342196
10.52	Ki	0.03	nM	CHEMBL3342334
10.41	Ki	0.039	nM	CHEMBL3926447
10.40	Ki	0.04	nM	CHEMBL3342198
10.40	Ki	0.04	nM	CHEMBL3699077
10.38	Ki	0.042	nM	CHEMBL3342192
10.36	Ki	0.044	nM	CHEMBL3891330
10.30	Ki	0.05	nM	CHEMBL3342195
10.28	Ki	0.053	nM	CHEMBL3950005
10.26	Ki	0.055	nM	NAVITOCLAX
10.22	Ki	0.06	nM	CHEMBL3699076
10.19	Ki	0.064	nM	CHEMBL3964082
10.10	Ki	0.08	nM	CHEMBL4465826
10.08	Ki	0.084	nM	CHEMBL3914582
10.00	Ki	0.1	nM	A-1155463
10.00	Ki	0.1	nM	CHEMBL3699066
10.00	Ki	0.1	nM	CHEMBL3699067
10.00	Ki	0.1	nM	CHEMBL3968862
10.00	Ki	0.1	nM	CHEMBL3923044
9.89	Kd	0.13	nM	ABT 737
9.85	Kd	0.14	nM	CHEMBL2398169
9.85	Ki	0.14	nM	CHEMBL3699075
9.85	Ki	0.14	nM	CHEMBL3699066
9.70	Ki	0.2	nM	CHEMBL3699079
9.70	Ki	0.2	nM	CHEMBL3939320
9.70	Ki	0.2	nM	CHEMBL3903275
9.70	Ki	0.2	nM	CHEMBL3900505
9.70	Ki	0.2	nM	CHEMBL4109874
9.70	Ki	0.2	nM	CHEMBL3971433
9.70	Ki	0.2	nM	CHEMBL3932865
9.70	Ki	0.2	nM	CHEMBL3930937
9.55	Ki	0.28	nM	CHEMBL3342197
9.53	Ki	0.296	nM	CHEMBL3972984
9.52	Ki	0.3	nM	CHEMBL3952597
9.52	Ki	0.3	nM	CHEMBL3901568
9.52	Ki	0.3	nM	CHEMBL3923784
9.52	Ki	0.3	nM	CHEMBL3938235
9.52	IC50	0.3	nM	ABT 737
9.51	Ki	0.307	nM	CHEMBL3923607
9.48	Ki	0.33	nM	CHEMBL3342334
9.48	Ki	0.329	nM	CHEMBL3901568
9.47	Ki	0.34	nM	CHEMBL3342190
9.43	Kd	0.37	nM	ABT 737
9.42	Ki	0.38	nM	CHEMBL3342192

PubChem BioAssay actives

1491 with measured affinity, of 2579 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
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-5-[3-[4-[4-[3-(4-methylpiperazin-1-yl)propylamino]pyrazolo[3,4-d]pyrimidin-1-yl]phenoxy]propyl]-1,3-thiazole-4-carboxylic acid	1168930: Inhibition of BCL-XL (unknown origin) incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-5-[3-(4-pyrazol-1-ylphenoxy)propyl]-1,3-thiazole-4-carboxylic acid	1168930: Inhibition of BCL-XL (unknown origin) incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-5-[3-[4-[4-[3-(dimethylamino)propylamino]pyrazolo[3,4-d]pyrimidin-1-yl]phenoxy]propyl]-1,3-thiazole-4-carboxylic acid	1168930: Inhibition of BCL-XL (unknown origin) incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-5-[3-(4-pyrazolo[3,4-d]pyrimidin-1-ylphenoxy)propyl]-1,3-thiazole-4-carboxylic acid	1168930: Inhibition of BCL-XL (unknown origin) incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-5-[3-[2-chloro-4-[3-(dimethylamino)prop-1-ynyl]phenoxy]propyl]-1,3-thiazole-4-carboxylic acid	1168930: Inhibition of BCL-XL (unknown origin) incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-5-[3-[4-[3-(dimethylamino)prop-1-ynyl]-2,5-difluorophenoxy]propyl]-1,3-thiazole-4-carboxylic acid	1168930: Inhibition of BCL-XL (unknown origin) incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-5-[3-[4-[3-(dimethylamino)prop-1-ynyl]phenoxy]propyl]-1,3-thiazole-4-carboxylic acid	1168930: Inhibition of BCL-XL (unknown origin) incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-5-[3-[4-[3-(dimethylamino)prop-1-ynyl]-3-fluorophenoxy]propyl]-1,3-thiazole-4-carboxylic acid	1168930: Inhibition of BCL-XL (unknown origin) incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-5-[3-[4-[3-(dimethylamino)prop-1-ynyl]-2-fluorophenoxy]propyl]-1,3-thiazole-4-carboxylic acid	1168930: Inhibition of BCL-XL (unknown origin) incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-(1-benzyl-3,5-dimethylpyrazol-4-yl)pyridine-2-carboxylic acid	1724940: Inhibition of F-Bak (GQVGRQLAIIGDK(6-FAM)INR-amide probe binding to BCL-xl (unknown origin) incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-(1-benzyl-5-methylpyrazol-4-yl)pyridine-2-carboxylic acid	1724940: Inhibition of F-Bak (GQVGRQLAIIGDK(6-FAM)INR-amide probe binding to BCL-xl (unknown origin) incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[1-(cyclohexylmethyl)-5-methylpyrazol-4-yl]pyridine-2-carboxylic acid	1724940: Inhibition of F-Bak (GQVGRQLAIIGDK(6-FAM)INR-amide probe binding to BCL-xl (unknown origin) incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
3-[1-(1-adamantylmethyl)-5-methylpyrazol-4-yl]-6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]pyridine-2-carboxylic acid	1293720: Binding affinity to Bcl-XL (unknown origin) by FRET assay	ki	<0.0001	uM
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-[1-[(3-methoxy-1-adamantyl)methyl]-5-methylpyrazol-4-yl]pyridine-2-carboxylic acid	1724940: Inhibition of F-Bak (GQVGRQLAIIGDK(6-FAM)INR-amide probe binding to BCL-xl (unknown origin) incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
4-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide	756752: Binding affinity to human GST-tagged Bcl-Xl assessed as dissociation rate by surface plasmon resonance assay	kd	0.0001	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,3S)-2-acetamido-3-methylpentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-5-amino-5-oxopentanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid	1931640: Binding affinity to recombinant His-tagged human Bcl-xL expressed in Escherichia coli assessed as inhibition constant by SPR analysis	ki	0.0001	uM
4-[4-[[2-(4-chlorophenyl)-5,5-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide	1388439: Inhibition of Bcl-xL (unknown origin)	ki	0.0001	uM
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-1,3-thiazole-4-carboxamide	1710463: Inhibition of F-Bak binding to GST-tagged BCL-XL (unknown origin) measured after 1 hr by TR-FRET assay	ki	0.0001	uM
(4S)-4-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[5-[(3aS,4S,6aR)-2-oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-4-yl]pentanoylamino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]amino]-5-[[(2S,3S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-5-carbamimidamido-1-[[(1S)-4-carbamimidamido-1-carboxybutyl]amino]-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid	756752: Binding affinity to human GST-tagged Bcl-Xl assessed as dissociation rate by surface plasmon resonance assay	kd	0.0001	uM
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-5-[3-(3-pyrazolo[3,4-d]pyrimidin-1-ylphenoxy)propyl]-1,3-thiazole-4-carboxylic acid	1168930: Inhibition of BCL-XL (unknown origin) incubated for 1 hr by TR-FRET assay	ki	0.0003	uM
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-(1-benzylpyrazol-4-yl)pyridine-2-carboxylic acid	1724940: Inhibition of F-Bak (GQVGRQLAIIGDK(6-FAM)INR-amide probe binding to BCL-xl (unknown origin) incubated for 1 hr by TR-FRET assay	ki	0.0003	uM
6-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-3-(1-benzylpyrrol-3-yl)pyridine-2-carboxylic acid	1724940: Inhibition of F-Bak (GQVGRQLAIIGDK(6-FAM)INR-amide probe binding to BCL-xl (unknown origin) incubated for 1 hr by TR-FRET assay	ki	0.0003	uM
2-[8-(1,3-benzothiazol-2-ylcarbamoyl)-3,4-dihydro-1H-isoquinolin-2-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonyl-1,3-thiazole-4-carboxamide	1710463: Inhibition of F-Bak binding to GST-tagged BCL-XL (unknown origin) measured after 1 hr by TR-FRET assay	ki	0.0004	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[2-methoxy-4-(3-morpholin-4-ylpropyl)phenyl]benzamide	260138: Binding affinity to Bcl-XL by fluorescence polarization assay	ki	0.0005	uM
N-[4-[[(2R)-6-(dimethylamino)-1-phenylsulfanylhexan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[2-methoxy-4-(3-morpholin-4-ylpropyl)phenyl]benzamide	260138: Binding affinity to Bcl-XL by fluorescence polarization assay	ki	0.0005	uM
4-[2-methoxy-4-(3-morpholin-4-ylpropyl)phenyl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide	260138: Binding affinity to Bcl-XL by fluorescence polarization assay	ki	0.0005	uM
4-[4-[(3-chlorophenyl)methyl]-4-methoxypiperidin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide	1798081: Fluorescence Polarization (FP) Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[4-methoxy-4-[(2-phenylphenyl)methyl]piperidin-1-yl]benzamide	1798081: Fluorescence Polarization (FP) Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[4-[(4-fluorophenyl)methylidene]piperidin-1-yl]benzamide	1798080: Fluorescence Polarization Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
4-[4-[(2-chlorophenyl)methylidene]piperidin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide	1798081: Fluorescence Polarization (FP) Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[4-[[2-(trifluoromethyl)phenyl]methylidene]piperidin-1-yl]benzamide	1798081: Fluorescence Polarization (FP) Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
4-[4-[(2-cyanophenyl)methylidene]piperidin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide	1798081: Fluorescence Polarization (FP) Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[4-[(2-methylsulfanylphenyl)methyl]piperazin-1-yl]benzamide	1798080: Fluorescence Polarization Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
4-[4-[(2-cyclohexylphenyl)methyl]piperazin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide	1798080: Fluorescence Polarization Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[4-[(2-phenylphenyl)methyl]piperazin-1-yl]benzamide	1798080: Fluorescence Polarization Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[4-[(2-pyridin-3-ylphenyl)methyl]piperazin-1-yl]benzamide	1798080: Fluorescence Polarization Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[4-[[2-(4-methoxyphenyl)phenyl]methyl]piperazin-1-yl]benzamide	1798080: Fluorescence Polarization Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
4-[4-[[2-(3-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide	1798080: Fluorescence Polarization Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[4-[[2-(4-fluorophenyl)phenyl]methyl]piperazin-1-yl]benzamide	1798080: Fluorescence Polarization Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[4-[[2-[4-(trifluoromethyl)phenyl]phenyl]methyl]piperazin-1-yl]benzamide	1798080: Fluorescence Polarization Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
4-[4-[(2-chlorophenyl)methyl]-4-methoxypiperidin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide	1798081: Fluorescence Polarization (FP) Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[4-methoxy-4-[(2-methylphenyl)methyl]piperidin-1-yl]benzamide	1798081: Fluorescence Polarization (FP) Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
4-[4-[(2-bromophenyl)methyl]-4-methoxypiperidin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide	1798081: Fluorescence Polarization (FP) Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[4-[(2-fluorophenyl)methylidene]piperidin-1-yl]benzamide	1798081: Fluorescence Polarization (FP) Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
4-[4-[(4-chlorophenyl)methylidene]piperidin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide	1798081: Fluorescence Polarization (FP) Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[4-[(2-phenylphenyl)methylidene]piperidin-1-yl]benzamide	1798080: Fluorescence Polarization Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[4-[(2-methoxyphenyl)methyl]piperazin-1-yl]benzamide	1798080: Fluorescence Polarization Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[4-[(2-morpholin-4-ylphenyl)methyl]piperazin-1-yl]benzamide	1798080: Fluorescence Polarization Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[4-[[2-(trifluoromethyl)phenyl]methyl]piperazin-1-yl]benzamide	1798080: Fluorescence Polarization Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-[4-[[2-(3-methoxyphenyl)phenyl]methyl]piperazin-1-yl]benzamide	1798080: Fluorescence Polarization Assay and FL5.12 Cellular Assay from Article 10.1021/jm061152t: “Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.”	ki	0.0005	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Arsenic Trioxide	decreases reaction, increases phosphorylation, decreases expression, affects expression, increases expression (+4 more)	33
Doxorubicin	affects response to substance, decreases reaction, increases activity, affects expression, affects reaction (+8 more)	22
Resveratrol	affects binding, affects cotreatment, affects reaction, increases activity, decreases response to substance (+6 more)	21
Cisplatin	decreases reaction, increases response to substance, increases reaction, increases expression, increases degradation (+3 more)	20
Curcumin	decreases reaction, increases expression, increases reaction, decreases expression, affects cotreatment (+1 more)	18
Fluorouracil	decreases expression, affects cotreatment, increases response to substance, decreases response to substance, increases reaction (+5 more)	18
Quercetin	affects cotreatment, decreases expression, affects binding, decreases reaction, increases reaction (+2 more)	17
Bortezomib	affects reaction, increases activity, increases cleavage, increases expression, increases response to substance (+4 more)	14
sodium arsenite	affects binding, affects cotreatment, affects reaction, decreases reaction, increases expression (+4 more)	12
Paclitaxel	decreases response to substance, decreases reaction, increases expression, affects cotreatment, decreases expression (+1 more)	12
Plant Extracts	affects cotreatment, decreases expression, decreases reaction, increases expression, increases abundance	11
(+)-JQ1 compound	affects cotreatment, decreases reaction, decreases expression, increases reaction, increases response to substance (+3 more)	10
Vorinostat	decreases expression, increases reaction, increases expression, decreases reaction, decreases response to substance (+1 more)	9
Acetylcysteine	affects cotreatment, increases phosphorylation, decreases expression, decreases reaction, increases expression	9
Estradiol	decreases expression, increases reaction, affects expression, increases expression	9
bisphenol A	increases reaction, decreases expression, affects cotreatment, affects expression, affects reaction (+1 more)	7
Sorafenib	decreases reaction, increases activity, increases cleavage, decreases expression, increases reaction (+2 more)	7
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one	affects cotreatment, decreases expression, decreases reaction, increases expression, increases degradation	6
pyrazolanthrone	affects cotreatment, decreases expression, decreases reaction, affects binding, increases phosphorylation	6
Dexamethasone	increases stability, decreases expression, decreases reaction, increases expression	6
Etoposide	decreases response to substance, affects expression, affects binding, increases expression, decreases reaction (+4 more)	6
Hydrogen Peroxide	decreases expression, decreases reaction, increases reaction, affects expression	6
Tretinoin	decreases expression, decreases reaction, increases reaction, affects cotreatment, increases expression	6
trichostatin A	decreases expression, decreases reaction, affects expression, increases reaction, affects cotreatment (+1 more)	5
Benzo(a)pyrene	increases abundance, decreases expression, increases expression, affects cotreatment	5
Cadmium	decreases reaction, affects expression, increases abundance, affects cotreatment, decreases expression (+4 more)	5
Niclosamide	decreases reaction, increases expression, decreases expression, increases reaction, affects binding	5
Arachidonic Acid	decreases expression, decreases reaction, affects cotreatment	5
Cadmium Chloride	decreases expression, affects expression, increases abundance, affects cotreatment, increases expression (+1 more)	5
Sirolimus	affects cotreatment, decreases expression, decreases reaction, increases expression	5

ChEMBL screening assays

495 unique, capped per target: 471 binding, 13 functional, 11 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1251000	Binding	Inhibition of GST-tagged Bel-xl/FITC-conjugated Bak interaction by fluorescence polarisation assay	Synthesis and biological activities of new di- and trimeric quinoline derivatives. — Bioorg Med Chem
CHEMBL2162642	Functional	Antagonist activity at recombinant Bcl-XL assessed as restoration of BIM BH3-induced cytochrome c release in mitochondria isolated from MDA-MB-231 cells at 0.03 to 1 uM after 1 hr by Western blot analysis	Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity. — J Med Chem
CHEMBL4023203	ADMET	Inhibition of FITC-Bak-BH3 binding to Bcl-XL (unknown origin) after 1.5 hrs by fluorescence polarization assay	Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors Using Structure-Based Design. — J Med Chem

Cellosaurus cell lines

19 cell lines: 12 transformed cell line, 7 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_1967	BLUE-1	Cancer cell line	Male
CVCL_9U00	HeLa ICRP Bcl-xL-mCherry	Cancer cell line	Female
CVCL_D590	SF-xL	Cancer cell line	Male
CVCL_D9W4	Ubigene HEL BCL2L1 KO	Cancer cell line	Male
CVCL_E6HV	K562(Bcl-xL)	Cancer cell line	Female
CVCL_HC61	Bcl-x-KO MEF Bcl-xL expressing	Transformed cell line	Sex unspecified
CVCL_KW13	InCELL Hunter U2OS BCL2L1-BAX Protein Binding	Cancer cell line	Female
CVCL_KW14	InCELL Hunter U2OS BCL2L1-BIM Protein Binding	Cancer cell line	Female
CVCL_T420	Psi-CRIP-RxBcl-XL-i-bsr	Transformed cell line	Male
CVCL_Y381	293XL/null	Transformed cell line	Female

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT02562170	PHASE4	COMPLETED	Protexa® Versus TiLoopBra® in Immediate Breast Reconstruction- A Pilot Study
NCT00673335	PHASE3	COMPLETED	Letrozole in Preventing Breast Cancer in Postmenopausal Women With a BRCA1 or BRCA2 Mutation
NCT00685256	PHASE3	COMPLETED	Standard Genetic Counseling With or Without a Decision Guide in Improving Communication Between Mothers Undergoing BRCA1/2 Testing and Their Minor-Age Children
NCT03162276	PHASE3	UNKNOWN	Trial of Inquiry Based Stress Reduction (IBSR) Program for BRCA1/2 Mutation Carriers
NCT00253539	PHASE2	COMPLETED	Arzoxifene or Tamoxifen in Preventing Breast Cancer in Premenopausal Women at High Risk for Breast Cancer
NCT00305695	PHASE2	COMPLETED	Zoledronate or Observation in Maintaining Bone Mineral Density in Patients Who Are Undergoing Surgery to Remove Both Ovaries
NCT00321633	PHASE2	COMPLETED	Carboplatin or Docetaxel in Treating Women With Metastatic Genetic Breast Cancer
NCT01333748	PHASE2	COMPLETED	Search Allelic Imbalance of Expression of BRCA Genes in Hereditary Risk of Breast and/or Ovarian Cancer
NCT01367639	PHASE2	COMPLETED	Trial of Inquiry Based Stress Reduction (IBSR) Program for BRCA1/2 Mutation Carriers
NCT00535119	PHASE1	COMPLETED	Veliparib, Carboplatin, and Paclitaxel in Treating Patients With Advanced Solid Cancer
NCT00892736	PHASE1	COMPLETED	Veliparib in Treating Patients With Malignant Solid Tumors That Do Not Respond to Previous Therapy
NCT03832985	EARLY_PHASE1	COMPLETED	Pediatric Reporting of Adult-Onset Genomic Results
NCT00005095	Not specified	RECRUITING	Specimen and Data Study for Ovarian Cancer Early Detection and Prevention
NCT00609505	Not specified	COMPLETED	Telemedicine vs. Face-to-Face Cancer Genetic Counseling
NCT01273909	Not specified	UNKNOWN	Outcomes After Perforator Flap Reconstruction for Breast Reconstruction and/or Lymphedema Treatment
NCT01445275	Not specified	WITHDRAWN	Cost of Cancer Risk Management in Women at Elevated Genetic Risk for Ovarian Cancer Who Participated on GOG-0199
NCT01608074	Not specified	ACTIVE_NOT_RECRUITING	Radical Fimbriectomy for Young BRCA Mutation Carriers
NCT02087592	Not specified	COMPLETED	Feasibility of Lifestyle Intervention in BRCA1/2 Mutation Carriers
NCT02302742	Not specified	RECRUITING	Triple Negative Breast Cancer and Germline Hereditary Breast and Ovarian Cancer Mutation Carrier Registry
NCT02324062	Not specified	COMPLETED	Cancer Genetics Hereditary Cancer Panel Testing
NCT02516540	Not specified	UNKNOWN	Efficacy of Lifestyle Intervention in BRCA1/2 Mutation Carriers
NCT02653105	Not specified	ACTIVE_NOT_RECRUITING	Women at Risk of Breast Cancer and OLFM4
NCT02705924	Not specified	TERMINATED	Impact of a Psychoeducational Intervention on Expectations and Coping in Young Women Exposed to a High HBOC Risk
NCT02760849	Not specified	ACTIVE_NOT_RECRUITING	Surgery in Preventing Ovarian Cancer in Patients With Genetic Mutations
NCT02786147	Not specified	COMPLETED	Identification and Referral of Women at Risk for Hereditary Breast/Ovarian Cancer
NCT02956681	Not specified	COMPLETED	Statewide Communication to Reach Diverse Low Income Women
NCT03015376	Not specified	UNKNOWN	Inherited Susceptible Genes Among Epithelial Ovarian Cancer
NCT03050268	Not specified	RECRUITING	Familial Investigations of Childhood Cancer Predisposition
NCT03075540	Not specified	COMPLETED	Enhancing At-risk Latina Women’s Use of Genetic Counseling for Hereditary Breast and Ovarian Cancer
NCT03124212	Not specified	RECRUITING	Cascade Genetic Testing for Hereditary Breast/Ovarian Cancer and Lynch Syndrome in Switzerland
NCT03246841	Not specified	ACTIVE_NOT_RECRUITING	Investigation of Tumour Spectrum of Germline Mutations in Breast and Ovarian Cancer Genes.
NCT03294343	Not specified	UNKNOWN	Risk-Reducing Surgeries for Hereditary Ovarian Cancer
NCT03421327	Not specified	COMPLETED	Genetic Risk: Whether, When, and How to Tell Adolescents
NCT03510689	Not specified	COMPLETED	Genetics and Heart Health After Cancer Therapy
NCT03511690	Not specified	COMPLETED	Testing an Intelligent Tutoring System to Enhance Genetic Risk Assessment
NCT03784859	Not specified	COMPLETED	Tissue Expansion in Breast Reconstruction Without Drains
NCT03979612	Not specified	UNKNOWN	Evaluation of the Adhesion to the GENEPY Network
NCT04197856	Not specified	ACTIVE_NOT_RECRUITING	Direct Information to At-risk Relatives
NCT04407611	Not specified	COMPLETED	Scalable Communication Modalities for Returning Genetic Research Results
NCT04508764	Not specified	TERMINATED	Implementation of the Families Accelerating Cascade Testing Toolkit (FACTT) for Hereditary Breast and Ovarian Cancer and Lynch Syndrome

Targeted by drugs: Navitoclax, Obatoclax, Venetoclax