BCL2A1

Summary

BCL2A1 (BCL2 related protein A1, HGNC:991) is a protein-coding gene on chromosome 15q25.1, encoding Bcl-2-related protein A1 (Q16548). Retards apoptosis induced by IL-3 deprivation.

This gene encodes a member of the BCL-2 protein family. The proteins of this family form hetero- or homodimers and act as anti- and pro-apoptotic regulators that are involved in a wide variety of cellular activities such as embryonic development, homeostasis and tumorigenesis. The protein encoded by this gene is able to reduce the release of pro-apoptotic cytochrome c from mitochondria and block caspase activation. This gene is a direct transcription target of NF-kappa B in response to inflammatory mediators, and is up-regulated by different extracellular signals, such as granulocyte-macrophage colony-stimulating factor (GM-CSF), CD40, phorbol ester and inflammatory cytokine TNF and IL-1, which suggests a cytoprotective function that is essential for lymphocyte activation as well as cell survival. Alternatively spliced transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 597 — RefSeq curated summary.

At a glance

• GWAS associations: 17
• Clinical variants (ClinVar): 25 total
• Druggable target: yes — 2 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_004049

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:991
Approved symbol	BCL2A1
Name	BCL2 related protein A1
Location	15q25.1
Locus type	gene with protein product
Status	Approved
Aliases	GRS, BFL1, BCL2L5, ACC-1, ACC-2, ACC2, ACC1
Ensembl gene	ENSG00000140379
Ensembl biotype	protein_coding
OMIM	601056
Entrez	597

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 3 protein_coding

ENST00000267953, ENST00000335661, ENST00000677151

RefSeq mRNA: 2 — MANE Select: NM_004049 NM_001114735, NM_004049

CCDS: CCDS10312, CCDS45322

Canonical transcript exons

ENST00000267953 — 2 exons

Exon	Start	End
ENSE00001104195	79970700	79971196
ENSE00001832143	79960892	79961174

Expression profiles

Bgee: expression breadth ubiquitous, 203 present calls, max score 99.10.

FANTOM5 (CAGE): breadth broad, TPM avg 112.9166 / max 22631.4870, expressed in 825 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
151192	94.0570	815
151193	8.6624	349
151190	8.4604	227
151191	1.7367	169

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
periodontal ligament	UBERON:0008266	99.10	gold quality
monocyte	CL:0000576	99.02	gold quality
mononuclear cell	CL:0000842	98.79	gold quality
leukocyte	CL:0000738	98.69	gold quality
granulocyte	CL:0000094	97.12	gold quality
bone marrow	UBERON:0002371	96.86	gold quality
right lung	UBERON:0002167	95.40	gold quality
bone marrow cell	CL:0002092	95.18	gold quality
spleen	UBERON:0002106	94.82	gold quality
vermiform appendix	UBERON:0001154	94.46	gold quality
upper lobe of left lung	UBERON:0008952	93.94	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	93.91	gold quality
blood	UBERON:0000178	93.85	gold quality
upper lobe of lung	UBERON:0008948	93.24	gold quality
cartilage tissue	UBERON:0002418	93.09	gold quality
lymph node	UBERON:0000029	92.38	gold quality
trabecular bone tissue	UBERON:0002483	87.09	gold quality
lung	UBERON:0002048	85.97	gold quality
caecum	UBERON:0001153	85.89	gold quality
lower lobe of lung	UBERON:0008949	84.60	gold quality
gall bladder	UBERON:0002110	83.25	gold quality
omental fat pad	UBERON:0010414	82.57	gold quality
peritoneum	UBERON:0002358	82.46	gold quality
adipose tissue of abdominal region	UBERON:0007808	81.77	gold quality
superficial temporal artery	UBERON:0001614	77.50	gold quality
rectum	UBERON:0001052	77.25	gold quality
right lobe of liver	UBERON:0001114	77.08	gold quality
palpebral conjunctiva	UBERON:0001812	77.01	gold quality
amniotic fluid	UBERON:0000173	76.92	gold quality
left uterine tube	UBERON:0001303	76.72	gold quality

Single-cell (SCXA)

Detected in 19 experiment(s), a significant marker in 18.

Experiment	Marker?	Max mean expression
E-GEOD-139324	yes	3034.15
E-GEOD-135922	yes	3032.22
E-HCAD-36	yes	2964.62
E-MTAB-6678	yes	2326.56
E-MTAB-6701	yes	1776.30
E-HCAD-15	yes	1475.44
E-HCAD-1	yes	100.35
E-CURD-122	yes	66.74
E-MTAB-9467	yes	34.37
E-CURD-46	yes	29.87
E-MTAB-9221	yes	28.66
E-MTAB-8142	yes	26.83
E-HCAD-10	yes	24.29
E-CURD-112	yes	22.41
E-CURD-88	yes	13.04

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AP1, CEBPB, EGR1, FOXL2, FOXO1, HDAC1, JUN, MITF, NFKB1, NFKB, REL, RELA, TCF3

miRNA regulators (miRDB)

13 targeting BCL2A1, 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-513B-5P	99.99	69.96	2150
HSA-MIR-548N	99.98	71.94	4170
HSA-MIR-587	99.64	70.86	2611
HSA-MIR-12123	99.52	71.79	2990
HSA-MIR-3123	99.47	67.15	2693
HSA-MIR-664A-3P	99.22	71.08	2696
HSA-MIR-518C-5P	98.53	69.20	1640
HSA-MIR-6810-5P	98.29	66.21	975
HSA-MIR-493-3P	97.50	66.44	731
HSA-MIR-514A-5P	96.94	65.49	801
HSA-MIR-382-5P	96.71	65.90	762
HSA-MIR-6514-5P	95.07	66.02	655
HSA-MIR-1295A	85.69	62.42	75

Literature-anchored findings (GeneRIF, showing 40)

• Bcl-2 family member Bfl-1/A1 sequesters truncated bid to inhibit is collaboration with pro-apoptotic Bak or Bax. (PMID:11929871)
• role for NF-kappa B in bfl-1 transcription (PMID:12665576)
• the level of Bfl-1 gene expression was higher in more advanced breast cancers than in early cancers; it seems that the increased expression of the Bfl-1 gene serves as a contributory factor in breast cancer in the same way that another group of genes (PMID:12692420)
• identification of two novel minor histocompatibility antigens, encoded by two separate single nucleotide polymorphisms on a single gene, BCL2A1, and restricted by HLA-A*2402 and B*4403 (PMID:12771180)
• Epstein Barr virus LMP1 drives bfl-1 promoter activity through interactions with components of the tumor necrosis factor receptor (TNFR)/CD40 signaling pathway; evidence presented that this process is NF-kappa B dependent (PMID:14747545)
• confers protection from hydrogen peroxide- and peroxynitrite- induced apoptosis in neutrophils and HL-60 cells (PMID:14966372)
• The expression of BCL2A1 was compared in two inbred strains of mice. (PMID:14981542)
• High expression of bfl-1 contributes to the apoptosis resistant phenotype in B-cell chronic lymphocytic leukemia (PMID:15499630)
• expression in urethral epithelium upregulated by Neisseria gonorrhoeae PorB IB and upregulation dependent on NF-kappaB activation (PMID:15501771)
• Oxidative stress induces the expression of Bfl-1 via NF-kappaB activation, and this early-response gene protects cells from Fas-mediated apoptosis. (PMID:15592513)
• results suggest that Anaplasma phagocytophilum inhibits human neutrophil apoptosis via transcriptional upregulation of bfl-1 and inhibition of mitochondria-mediated activation of caspase 3 (PMID:15617521)
• performed a Bfl-1 deletion study in order to elucidate the underlying mechanism of GFP-Bfl-1-induced cell death (PMID:15696550)
• A1 and A20 are both required for optimal protection from apoptosis (A1) and inflammation (A20) in conditions leading to renal damage (PMID:16164629)
• The C terminus of A1 did not function as a membrane anchor; it serves a dual function by controlling the stability of A1 and by amplifying the capacity of the protein to protect cells against apoptosis. (PMID:16551634)
• Bfl-1/A1 mRNA is not expressed in these cell lines, however, its expression is markedly induced by ATRA treatment in NB4 and HL-60 cells, but not in R4 or HL-60/Res cells, which correlates with inhibition of apoptosis. (PMID:16572199)
• EBNA2 trans-activates bfl-1, which requires CBF1 (or RBP-J kappa). (PMID:16873269)
• the known polymorphisms of exon 1 and a novel polymorphism in the promoter region provide evidence for an association between bfl-1 polymorphisms and genetic predisposition to atopic dermatitis (PMID:17121585)
• Amphipathic tail-anchoring peptide (ATAP) targets specifically to mitochondria, and induces caspase-dependent apoptosis that does not require Bax or Bak. (PMID:17666431)
• Bfl-1 associates with tBid to prevent activation of proapoptotic Bax and Bak, and it also interacts directly with Bak to antagonize Bak-mediated cell death, similar to myeloid cell factor (Mcl)-1. (PMID:17724464)
• Specific downregulation of bfl-1 using siRNA induced apoptosis in resistant cells. Our data suggest that bfl-1 contributes to chemoresistance and might be a therapeutic target in B-CLL. (PMID:17726463)
• While TNFalpha had no effect on MCL-1 transcription, it induced expression of another antiapoptotic molecule, BFL-1. (PMID:17942758)
• Results clearly indicated that differential expression of bfl-1/A1 in M. tuberculosis H37Rv and M. tuberculosis H37Ra infected THP-1 cells probably account for the difference in infection outcome. (PMID:18206119)
• targeting mHags encoded not only by HMHA1, whose aberrant expression in solid tumors has been reported, but also BCL2A1 may bring about beneficial selective graft-versus-tumor effects (PMID:18414982)
• C/EBP beta overexpression significantly upregulated promoter activities of IL-8, COX-2, and anti-apoptotic Bfl-1 genes in prostate cancer cells. (PMID:18512730)
• The crystal structure of Bfl-1, the last anti-apoptotic Bcl-2 family member to be structurally characterized, in complex with a peptide corresponding to the BH3 region of the pro-apoptotic protein Bim is presented. (PMID:18812174)
• the amphipathic character of Bfl-1 C-terminal helix alpha9 is required for the anchorage of Bfl-1 to the mitochondria and regulation the antiapoptotic function Bfl-1 (PMID:19759007)
• Defective ubiquitin-mediated degradation of antiapoptotic Bfl-1 predisposes to lymphoma. (PMID:20185581)
• Bfl-1/A1 negatively regulates autophagy and expression of Bfl-1/A1 in H37Rv infected macrophages (PMID:21167304)
• These findings are the first indication that Bfl-1 plays a crucial role in setting the elevated threshold of resistance of this malignant cell type to apoptosis (PMID:21491422)
• Bfl-1 importantly regulates lung cancer cell sensitivity to gemcitabine. (PMID:21843371)
• neutrophils from patients with sepsis express reduced levels of antiapoptotic Mcl1 and A1 (PMID:22231730)
• Inhibition of Mcl-1 and A1 strongly induced cell death in some melanoma cell lines. (PMID:22292048)
• The transcription factor Spi-B regulates human plasmacytoid dendritic cell survival through direct induction of the antiapoptotic gene BCL2-A1. (PMID:22510878)
• results directly implicate Bfl-1 and Bcl-x(L) in HTLV-1-infected T-cell survival and suggest that both Bfl-1 and Bcl-x(L) represent potential therapeutic targets for ATLL treatment. (PMID:22553204)
• results highlight Bfl-1 as a major effector in activation-induced human mast cell survival (PMID:22720045)
• Data demonstrate that calpain-mediated cleavage of full-length Bfl-1 induces the release of C-terminal membrane active alpha-helices that are responsible for its conversion into a pro-apoptotic factor. (PMID:22745672)
• Data indicate that BCL2a1 expression enhances tumor cell survival in nervous system (CNS) leading to intracranial tumor growth. (PMID:22865454)
• Bcl2a1 should be considered as a proto-oncogene with a potential role in both lymphoid and myeloid leukemogenesis (PMID:23118966)
• Mitochondrial antiapoptotic factor Bfl-1 is significantly reduced by suppressor of cytokine signaling (SOCS)1. (PMID:23152563)
• MITF-BCL2A1 as a lineage-specific oncogenic pathway in melanoma and underscore its role for improved response to BRAF-directed therapy. (PMID:23447565)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
mus_musculus	Bcl2a1c	ENSMUSG00000053820
mus_musculus	Bcl2a1b	ENSMUSG00000089929
mus_musculus	Bcl2a1d	ENSMUSG00000099974
mus_musculus	Bcl2a1a	ENSMUSG00000102037
rattus_norvegicus	Bcl2a1	ENSRNOG00000047606
caenorhabditis_elegans		WBGENE00000423

Paralogs (8): BAK1 (ENSG00000030110), BAX (ENSG00000087088), BCL2L2 (ENSG00000129473), BCL2L10 (ENSG00000137875), MCL1 (ENSG00000143384), BCL2L1 (ENSG00000171552), BCL2 (ENSG00000171791), BOK (ENSG00000176720)

Protein

Protein identifiers

Bcl-2-related protein A1 — Q16548 (reviewed: Q16548)

Alternative names: Bcl-2-like protein 5, Hemopoietic-specific early response protein, Protein BFL-1, Protein GRS

All UniProt accessions (2): Q16548, B4E1X9

UniProt curated annotations — full annotation on UniProt →

Function. Retards apoptosis induced by IL-3 deprivation. May function in the response of hemopoietic cells to external signals and in maintaining endothelial survival during infection. Can inhibit apoptosis induced by serum starvation in the mammary epithelial cell line HC11.

Subunit / interactions. Interacts directly with BAK1, BID, BMF and BBC3. Interacts directly with BCL2L11/BIM. Interacts with BAX isoform Sigma. Interacts directly with PMAIP1. Interacts with RTL10/BOP. Interacts with ING4. Interacts with UBQLN4.

Subcellular location. Cytoplasm.

Tissue specificity. Seems to be restricted to the hematopoietic compartment. Expressed in peripheral blood, spleen, and bone marrow, at moderate levels in lung, small intestine and testis, at a minimal levels in other tissues. Also found in vascular smooth muscle cells and hematopoietic malignancies.

Induction. By phorbol ester and inflammatory cytokines, such as TNF or IL1B/interleukin-1 beta, but not by growth factors.

Similarity. Belongs to the Bcl-2 family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q16548-1	1	yes
Q16548-2	2

RefSeq proteins (2): NP_001108207, NP_004040* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002475	Bcl2-like	Family
IPR013282	Bcl2A1	Family
IPR020717	Bcl2_BH1_motif_CS	Conserved_site
IPR020726	Bcl2_BH2_motif_CS	Conserved_site
IPR026298	Bcl-2_fam	Family
IPR036834	Bcl-2-like_sf	Homologous_superfamily
IPR046371	Bcl-2_BH1-3	Domain

Pfam: PF00452

UniProt features (21 total): helix 9, sequence variant 4, short sequence motif 2, sequence conflict 2, chain 1, strand 1, turn 1, splice variant 1

Structure

Experimental structures (PDB)

26 structures.

PDB	Method	Resolution (Å)
9GIR	X-RAY DIFFRACTION	1.07
9GIT	X-RAY DIFFRACTION	1.15
5UUK	X-RAY DIFFRACTION	1.2
5UUL	X-RAY DIFFRACTION	1.33
9GIS	X-RAY DIFFRACTION	1.39
9GIQ	X-RAY DIFFRACTION	1.42
9S6M	X-RAY DIFFRACTION	1.43
9GIP	X-RAY DIFFRACTION	1.46
6E3I	X-RAY DIFFRACTION	1.48
6E3J	X-RAY DIFFRACTION	1.48
9EW8	X-RAY DIFFRACTION	1.49
9FKY	X-RAY DIFFRACTION	1.56
6MBB	X-RAY DIFFRACTION	1.59
9FKZ	X-RAY DIFFRACTION	1.68
5WHI	X-RAY DIFFRACTION	1.69
5UUP	X-RAY DIFFRACTION	1.73
6VO4	X-RAY DIFFRACTION	1.74
6MBC	X-RAY DIFFRACTION	1.75
8RPO	X-RAY DIFFRACTION	1.79
4ZEQ	X-RAY DIFFRACTION	1.8
9FL0	X-RAY DIFFRACTION	1.94
2VM6	X-RAY DIFFRACTION	2.2
3I1H	X-RAY DIFFRACTION	2.2
3MQP	X-RAY DIFFRACTION	2.24
5WHH	X-RAY DIFFRACTION	2.38
6RJP	X-RAY DIFFRACTION	2.57

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q16548-F1	87.63	0.65

Function

Pathways and Gene Ontology

Reactome pathways

9 pathways

ID	Pathway
R-HSA-9725371	Nuclear events stimulated by ALK signaling in cancer
R-HSA-9824594	Regulation of MITF-M-dependent genes involved in apoptosis
R-HSA-1266738	Developmental Biology
R-HSA-1643685	Disease
R-HSA-5663202	Diseases of signal transduction by growth factor receptors and second messengers
R-HSA-9700206	Signaling by ALK in cancer
R-HSA-9725370	Signaling by ALK fusions and activated point mutants
R-HSA-9730414	MITF-M-regulated melanocyte development
R-HSA-9856651	MITF-M-dependent gene expression

MSigDB gene sets: 453 (showing top): PID_BCR_5PATHWAY, FERRANDO_TAL1_NEIGHBORS, TONKS_TARGETS_OF_RUNX1_RUNX1T1_FUSION_MONOCYTE_UP, WALLACE_PROSTATE_CANCER_RACE_UP, BUYTAERT_PHOTODYNAMIC_THERAPY_STRESS_DN, SHIPP_DLBCL_VS_FOLLICULAR_LYMPHOMA_UP, MCLACHLAN_DENTAL_CARIES_UP, MODULE_169, MODULE_45, GOBP_EXTRINSIC_APOPTOTIC_SIGNALING_PATHWAY, DARWICHE_SKIN_TUMOR_PROMOTER_DN, DARWICHE_PAPILLOMA_RISK_LOW_DN, DARWICHE_PAPILLOMA_RISK_HIGH_DN, DARWICHE_SQUAMOUS_CELL_CARCINOMA_DN, BRUECKNER_TARGETS_OF_MIRLET7A3_DN

GO Biological Process (9): release of cytochrome c from mitochondria (GO:0001836), mitochondrial fusion (GO:0008053), intrinsic apoptotic signaling pathway in response to DNA damage (GO:0008630), positive regulation of apoptotic process (GO:0043065), negative regulation of apoptotic process (GO:0043066), extrinsic apoptotic signaling pathway in absence of ligand (GO:0097192), apoptotic process (GO:0006915), regulation of apoptotic process (GO:0042981), transmembrane transport (GO:0055085)

GO Molecular Function (2): channel activity (GO:0015267), protein binding (GO:0005515)

GO Cellular Component (3): cytoplasm (GO:0005737), mitochondrial outer membrane (GO:0005741), cytosol (GO:0005829)

Reactome top-level categories

Rollup of top-7 pathways:

Category	Pathways
Signaling by ALK fusions and activated point mutants	1
MITF-M-dependent gene expression	1
Disease	1
Diseases of signal transduction by growth factor receptors and second messengers	1
Signaling by ALK in cancer	1
Developmental Biology	1
MITF-M-regulated melanocyte development	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
apoptotic process	3
apoptotic signaling pathway	2
regulation of apoptotic process	2
cellular anatomical structure	2
apoptotic mitochondrial changes	1
mitochondrion organization	1
organelle fusion	1
DNA damage response	1
intrinsic apoptotic signaling pathway	1
positive regulation of programmed cell death	1
negative regulation of programmed cell death	1
signal transduction in absence of ligand	1
extrinsic apoptotic signaling pathway	1
programmed cell death	1
execution phase of apoptosis	1
regulation of programmed cell death	1
transport	1
cellular process	1
passive transmembrane transporter activity	1
binding	1
intracellular anatomical structure	1
mitochondrial membrane	1
organelle outer membrane	1
cytoplasm	1

Protein interactions and networks

STRING

2434 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
BCL2A1	PMAIP1	Q13794	995
BCL2A1	BCL2L11	O43521	985
BCL2A1	HSP90AA1	P07900	932
BCL2A1	HRK	O00198	919
BCL2A1	HSP90AB1	P08238	911
BCL2A1	FKBP5	Q13451	891
BCL2A1	BCL2L10	Q9HD36	848
BCL2A1	BIK	Q13323	831
BCL2A1	CRH	P06850	772
BCL2A1	BMF	Q96LC9	755
BCL2A1	POMC	P01189	739
BCL2A1	STAT5A	P42229	734
BCL2A1	STAT5B	P51692	728
BCL2A1	ALK	Q9UM73	708
BCL2A1	BAK1	Q16611	702

IntAct

35 interactions, top by confidence:

A	B	Type	Score
BIK	BCL2A1	psi-mi:“MI:0915”(physical association)	0.780
BCL2A1	BIK	psi-mi:“MI:0915”(physical association)	0.780
BCL2A1	BAK1	psi-mi:“MI:0915”(physical association)	0.720
BCL2A1	BCL2L11	psi-mi:“MI:0407”(direct interaction)	0.680
BCL2L11	BCL2A1	psi-mi:“MI:0915”(physical association)	0.680
FAM9B	BCL2A1	psi-mi:“MI:0915”(physical association)	0.560
BCL2A1	FAM9B	psi-mi:“MI:0915”(physical association)	0.560
BCL2A1	CT45A1	psi-mi:“MI:0915”(physical association)	0.560
BCL2A1	NHERF1	psi-mi:“MI:0915”(physical association)	0.490
BID	BCL2A1	psi-mi:“MI:0407”(direct interaction)	0.440
BCL2A1	BBC3	psi-mi:“MI:0407”(direct interaction)	0.440
BCL2A1	RTL10	psi-mi:“MI:0915”(physical association)	0.400
NR4A1	BCL2A1	psi-mi:“MI:0915”(physical association)	0.400
	BCL2A1	psi-mi:“MI:0915”(physical association)	0.400
	BCL2A1	psi-mi:“MI:0915”(physical association)	0.370
BCL2A1	BIK	psi-mi:“MI:0915”(physical association)	0.000
BCL2A1	BAK1	psi-mi:“MI:0915”(physical association)	0.000
BIK	BCL2A1	psi-mi:“MI:0915”(physical association)	0.000
BCL2A1	CT45A1	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (39): NR4A1 (Affinity Capture-Western), BCL2A1 (Two-hybrid), BIK (Two-hybrid), FAM9B (Two-hybrid), BID (Protein-peptide), BCL2L11 (Protein-peptide), BBC3 (Protein-peptide), BCL2A1 (Two-hybrid), BCL2A1 (Two-hybrid), BAD (Two-hybrid), BCL2A1 (Protein-peptide), BMF (Protein-peptide), BAD (Protein-peptide), PMAIP1 (Protein-peptide), BIK (Protein-peptide)

ESM2 similar proteins: A8WWR3, B3M1F2, B4HJA7, B4JSL2, B4M686, B4N8G7, B4QVV3, B6EU02, F1QYC4, F5HGJ3, G5ED05, O14017, O36423, O74371, P03182, P0C6Z1, P0C736, P41879, P41957, P41958, P90859, Q01001, Q07440, Q08ED0, Q09292, Q0II48, Q10436, Q16548, Q39162, Q3C2I0, Q4E409, Q4QFY1, Q5TBC7, Q66610, Q6GZM8, Q6VZT9, Q751B5, Q75BE5, Q77PA8, Q8IMZ9

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

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
RELA	“up-regulates quantity by expression”	BCL2A1	“transcriptional regulation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	20
Likely benign	0
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

341 predictions. Top by Δscore:

Variant	Effect	Δscore
15:79961170:TTTTC:T	acceptor_gain	1.0000
15:79961172:TTCC:T	acceptor_loss	1.0000
15:79961173:TCC:T	acceptor_loss	1.0000
15:79961176:T:C	acceptor_loss	1.0000
15:79970702:AG:A	donor_gain	1.0000
15:79961171:TTTC:T	acceptor_gain	0.9900
15:79961172:TTC:T	acceptor_gain	0.9900
15:79961175:C:CC	acceptor_gain	0.9900
15:79969213:A:AC	donor_gain	0.9900
15:79969214:C:CC	donor_gain	0.9900
15:79970696:ATACC:A	donor_loss	0.9900
15:79970697:TACCC:T	donor_loss	0.9900
15:79970698:A:AC	donor_gain	0.9900
15:79970698:AC:A	donor_gain	0.9900
15:79970698:ACCC:A	donor_loss	0.9900
15:79970699:C:CA	donor_loss	0.9900
15:79970699:C:CC	donor_gain	0.9900
15:79970699:CC:C	donor_gain	0.9900
15:79970699:CCCAG:C	donor_gain	0.9900
15:79970702:AGCCT:A	donor_gain	0.9900
15:79970714:G:A	donor_gain	0.9900
15:79970719:AT:A	donor_gain	0.9900
15:79970720:T:C	donor_gain	0.9900
15:79970770:T:TA	donor_gain	0.9900
15:79961173:TC:T	acceptor_gain	0.9800
15:79961174:CC:C	acceptor_gain	0.9800
15:79970694:ACAT:A	donor_loss	0.9800
15:79970706:T:TA	donor_gain	0.9800
15:79961175:CTAT:C	acceptor_gain	0.9600
15:79961176:T:G	acceptor_gain	0.9400

AlphaMissense

1150 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
15:79970864:A:G	W86R	0.981
15:79970864:A:T	W86R	0.981
15:79970702:A:G	W140R	0.977
15:79970702:A:T	W140R	0.977
15:79970862:C:A	W86C	0.976
15:79970862:C:G	W86C	0.976
15:79970700:C:A	W140C	0.972
15:79970700:C:G	W140C	0.972
15:79970856:T:A	R88S	0.960
15:79970856:T:G	R88S	0.960
15:79970723:A:G	W133R	0.959
15:79970723:A:T	W133R	0.959
15:79961151:A:C	F148L	0.957
15:79961151:A:T	F148L	0.957
15:79961153:A:G	F148L	0.957
15:79970883:A:C	F79L	0.957
15:79970883:A:T	F79L	0.957
15:79970885:A:G	F79L	0.957
15:79970745:G:C	F125L	0.951
15:79970745:G:T	F125L	0.951
15:79970747:A:G	F125L	0.951
15:79970721:C:A	W133C	0.950
15:79970721:C:G	W133C	0.950
15:79961163:A:C	F144L	0.949
15:79961163:A:T	F144L	0.949
15:79961165:A:G	F144L	0.949
15:79970701:C:G	W140S	0.948
15:79970857:C:G	R88T	0.931
15:79970841:A:C	F93L	0.927
15:79970841:A:T	F93L	0.927

dbSNP variants (sampled 300 via entrez): RS1000068662 (15:79972100 C>A,T), RS1000456148 (15:79967246 T>C), RS1000617147 (15:79960944 C>T), RS1001143053 (15:79966936 G>A), RS1001238264 (15:79972563 G>A), RS1001269422 (15:79972827 C>A,G,T), RS1001711882 (15:79965999 G>A,C), RS1001799893 (15:79961943 A>G), RS1002235827 (15:79961334 C>T), RS1002791736 (15:79963063 C>A), RS1002871052 (15:79964426 G>A,C,T), RS1003098299 (15:79964938 T>C), RS1003237279 (15:79963044 C>T), RS1003671029 (15:79969671 G>A), RS1003871104 (15:79969275 G>A,T)

Disease associations

OMIM: gene MIM:601056 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

17 associations (top):

Study	Trait	p-value
GCST004030_25	Primary sclerosing cholangitis	1.000000e-06
GCST004600_51	Eosinophil percentage of white cells	3.000000e-14
GCST004606_85	Eosinophil count	2.000000e-18
GCST004608_201	Granulocyte percentage of myeloid white cells	2.000000e-70
GCST004609_218	Monocyte percentage of white cells	6.000000e-97
GCST004617_158	Eosinophil percentage of granulocytes	3.000000e-16
GCST004623_72	Neutrophil percentage of granulocytes	2.000000e-13
GCST004624_161	Sum eosinophil basophil counts	3.000000e-16
GCST004625_155	Monocyte count	5.000000e-103
GCST005973_12	White blood cell count	3.000000e-16
GCST005975_20	Eosinophil count	2.000000e-10
GCST005977_15	Monocyte count	3.000000e-08
GCST90002381_630	Eosinophil count	4.000000e-21
GCST90002381_631	Eosinophil count	2.000000e-09
GCST90002382_327	Eosinophil percentage of white cells	9.000000e-22
GCST90002393_260	Monocyte count	4.000000e-209
GCST90002394_524	Monocyte percentage of white cells	7.000000e-197

EFO canonical traits (8, from GWAS)

EFO ID	Trait name
EFO:0007991	eosinophil percentage of leukocytes
EFO:0004842	eosinophil count
EFO:0007997	granulocyte percentage of myeloid white cells
EFO:0007989	monocyte percentage of leukocytes
EFO:0007996	eosinophil percentage of granulocytes
EFO:0007994	neutrophil percentage of granulocytes
EFO:0005090	basophil count
EFO:0005091	monocyte count

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (6): CHEMBL3885514 (PROTEIN-PROTEIN INTERACTION), CHEMBL3885524 (PROTEIN COMPLEX), CHEMBL5169268 (PROTEIN-PROTEIN INTERACTION), CHEMBL5169269 (PROTEIN-PROTEIN INTERACTION), CHEMBL5169270 (PROTEIN-PROTEIN INTERACTION), CHEMBL6044 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 25,718 (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
CHEMBL297453	EPIGALOCATECHIN GALLATE	3	22,804
CHEMBL408194	OBATOCLAX	3	2,914

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

Binding affinities (BindingDB)

217 measured of 225 human assays (234 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
2-Amino-4-benzo[1,3]dioxol-5-yl-6-(5-methyl-furan-2-yl)-nicotinonitrile	EC50	0.0206 nM
ABT-199	IC50	4.4 nM
130E7	IC50	27 nM
Apogossypol derivative, 8n	IC50	150 nM
2,5-bis(chloranyl)-3-(4-methylpiperazin-1-yl)-6-(2-piperidin-1-yl-1,3-thiazol-5-yl)cyclohexa-2,5-diene-1,4-dione	EC50	160 nM
2-chloranyl-3-[[4-(diethylamino)phenyl]amino]naphthalene-1,4-dione	EC50	170 nM
130D11	IC50	199 nM
US8937193, 8c	IC50	210 nM	US-8937193: Apogossypolone derivatives as anticancer agents
2,5-bis(chloranyl)-3-[2-(dimethylamino)-1,3-thiazol-5-yl]-6-pyrrolidin-1-yl-cyclohexa-2,5-diene-1,4-dione	EC50	210 nM
US8937193, 7	IC50	220 nM	US-8937193: Apogossypolone derivatives as anticancer agents
US8937193, 8a	IC50	230 nM	US-8937193: Apogossypolone derivatives as anticancer agents
US8937193, 6b	IC50	250 nM	US-8937193: Apogossypolone derivatives as anticancer agents
US8937193, 6i	IC50	290 nM	US-8937193: Apogossypolone derivatives as anticancer agents
Apogossypol derivative, 8r	IC50	320 nM
SMR000196363	EC50	320 nM
US8937193, 6l	IC50	340 nM	US-8937193: Apogossypolone derivatives as anticancer agents
US8937193, 6a	IC50	370 nM	US-8937193: Apogossypolone derivatives as anticancer agents
Apogossypol derivative, 12e	IC50	480 nM
Apogossypol derivative, 8k	IC50	490 nM
ethyl 2-[[(5Z)-5-[(4-bromophenyl)methylidene]-4-oxo-1,3-thiazol-2-yl]sulfanyl]acetate	EC50	550 nM
SMR000285999	EC50	560 nM
3-chloro-4-(3-methoxyphenoxy)-1-(4-methoxyphenyl)-1H-pyrrole-2,5-dione	EC50	610 nM
3-chloro-4-[(1,5-dimethyl-3-oxo-2-phenylpyrazolidin-4-yl)amino]-1-(4-methoxyphenyl)pyrrole-2,5-dione	EC50	620 nM
Apogossypol derivative, 8q	IC50	670 nM
cid_2135733	EC50	680 nM
Apogossypol derivative, 8s	IC50	700 nM
Apogossypol derivative, 8m	IC50	710 nM
(5Z)-5-{[4-(dimethylamino)phenyl]imino}-1-(3-hydroxypropyl)-4-methyl-2,6-dioxo-1,2,5,6-tetrahydropyridine-3-carbonitrile	EC50	760 nM
SMR000104797	EC50	850 nM
SMR000293370	EC50	850 nM
MLS001001946	EC50	920 nM
4-({(4Z)-1-oxo-4-[(phenylsulfonyl)imino]-1,4-dihydronaphthalen-2-yl}amino)benzoic acid	IC50	967 nM
MLS000708819	EC50	970 nM
MLS000571745	EC50	980 nM
MLS001006773	EC50	1090 nM
N-[5-[(4-chloranylphenoxy)methyl]-1,3,4-thiadiazol-2-yl]furan-2-carboxamide	EC50	1460 nM
2-(2-bromo-6-methoxy-4-{[(2-oxo-2,3-dihydro-1H-benzimidazol-5-yl)amino]methyl}phenoxy)-N-(tert-butyl)acetamide	EC50	1470 nM
cid_2135732	EC50	1580 nM
5-[4-(dimethylamino)phenyl]imino-1-(2-hydroxyethyl)-2,6-diketo-4-methyl-nicotinonitrile	EC50	1630 nM
SMR000207032	EC50	1630 nM
6-methyl-2-(1-naphthalenyl)-5-benzotriazolamine	EC50	1750 nM
MLS000374649	EC50	1770 nM
MLS000537607	EC50	1800 nM
MLS001007244	EC50	1840 nM
6-Methoxy-1,3-dimethyl-1H-benzo[de]cinnoline	EC50	2010 nM
3-(4-methylphenyl)-5-(4-morpholinyl)-2-phenyl-1,2,4-thiadiazol-2-ium	EC50	2040 nM
2-[[(5Z)-5-[(4-methoxyphenyl)methylidene]-4-oxo-2-thiazolyl]thio]acetic acid ethyl ester	EC50	2060 nM
(E)-3-(5-methyl-2-furanyl)-N-[3-[[(E)-3-(5-methyl-2-furanyl)-1-oxoprop-2-enyl]amino]-4-nitrophenyl]-2-propenamide	IC50	2120 nM
US8937193, 6g	IC50	2170 nM	US-8937193: Apogossypolone derivatives as anticancer agents
2-[1-[(Z)-1-(4-methoxyphenyl)-3-oxidanylidene-3-thiophen-2-yl-prop-1-en-2-yl]pyridin-2-ylidene]propanedinitrile	EC50	2230 nM

ChEMBL bioactivities

293 potent at pChembl≥5 of 333 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.41	IC50	3.9	nM	CHEMBL6147022
8.38	IC50	4.2	nM	CHEMBL6102509
8.35	IC50	4.5	nM	CHEMBL6146278
8.30	IC50	5	nM	CHEMBL6142882
8.27	IC50	5.4	nM	CHEMBL6091960
8.19	IC50	6.5	nM	CHEMBL4747465
8.18	IC50	6.6	nM	CHEMBL4782684
8.07	IC50	8.5	nM	CHEMBL3883565
8.07	IC50	8.5	nM	CHEMBL6143694
8.07	IC50	8.5	nM	CHEMBL6102150
8.00	Ki	10	nM	CHEMBL4782684
8.00	IC50	10	nM	CHEMBL6102006
7.96	IC50	11	nM	CHEMBL6083140
7.87	IC50	13.5	nM	CHEMBL4755711
7.87	IC50	13.4	nM	CHEMBL4791348
7.85	IC50	14	nM	CHEMBL6145269
7.77	IC50	17	nM	CHEMBL6120357
7.75	IC50	18	nM	CHEMBL5075478
7.75	IC50	18	nM	CHEMBL6146521
7.72	IC50	19	nM	CHEMBL6108907
7.69	IC50	20.4	nM	CHEMBL4752520
7.66	IC50	22	nM	CHEMBL5613766
7.64	EC50	23	nM	CHEMBL5281728
7.62	IC50	24	nM	CHEMBL6147348
7.54	IC50	29	nM	CHEMBL6141601
7.52	Ki	30.5	nM	CHEMBL4747465
7.51	IC50	30.9	nM	CHEMBL4465826
7.51	IC50	31	nM	CHEMBL6145093
7.51	IC50	31	nM	CHEMBL6078737
7.50	Ki	32	nM	CHEMBL3884841
7.48	IC50	33	nM	CHEMBL6133524
7.48	IC50	33	nM	CHEMBL6102527
7.40	IC50	40	nM	CHEMBL6102754
7.37	IC50	43	nM	CHEMBL6145783
7.33	Ki	46.7	nM	CHEMBL4752520
7.32	IC50	48	nM	CHEMBL6103426
7.30	IC50	50	nM	CHEMBL6120370
7.26	IC50	54.6	nM	CHEMBL4740212
7.20	IC50	63	nM	CHEMBL5613621
7.13	IC50	74	nM	CHEMBL6102979
7.12	IC50	75	nM	CHEMBL6141873
7.11	IC50	77	nM	CHEMBL6133700
7.09	Ki	81.6	nM	CHEMBL4755711
7.08	Ki	84	nM	CHEMBL4522193
7.08	IC50	83	nM	CHEMBL5613621
7.06	IC50	87	nM	CHEMBL6132659
7.05	IC50	90	nM	CHEMBL6087337
7.00	Ki	100	nM	CHEMBL4576854
7.00	Ki	100	nM	CHEMBL4533559
6.98	Ki	105	nM	CHEMBL5523629

PubChem BioAssay actives

265 with measured affinity, of 541 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
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,3S)-2-acetamido-3-methylpentanoyl]amino]-3-(prop-2-enoylamino)propanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-5-amino-5-oxopentanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(3S,9S,12S,21S)-21-[[(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]carbamoyl]-9-[(2S)-butan-2-yl]-3-(carboxymethyl)-12,21-dimethyl-2,5,8,11-tetraoxo-1,4,7,10-tetrazacyclohenicos-16-en-12-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid	1337035: Inhibition of FITC-betaA-DIIRNIARHLAQVGDSMRSI-NH2 binding to recombinant human Bcl2A1 (1 to 152 residues) BH3 binding site expressed in Escherichia coli measured after 2 hrs by fluorescence polarization assay	ki	0.0001	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[2-acetamido-3-[(2-chloroacetyl)amino]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	1802502: DELFIA from Article 10.1021/acschembio.6b00962: “hBfl-1/hNOXA Interaction Studies Provide New Insights on the Role of Bfl-1 in Cancer Cell Resistance and for the Design of Novel Anticancer Agents.”	kd	0.0026	uM
(4S)-4-[[(5S,8S,11S,19S)-19-acetamido-5-[(2S)-butan-2-yl]-8-methyl-3,6,9,13,20-pentaoxo-2-[(prop-2-enoylamino)methyl]-1,4,7,10,14-pentazacycloicosane-11-carbonyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S,8S,11S,19S)-11-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]carbamoyl]-2-[(2S)-butan-2-yl]-8-(carboxymethyl)-3,6,9,13,20-pentaoxo-1,4,7,10,14-pentazacycloicos-19-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid	1715809: Binding affinity to human Bcl2A1 incubated for 2 hrs by FBid based competitive FP assay	ic50	0.0065	uM
(4S)-4-[[(5S,8S,11S,15E,20S)-20-acetamido-5-[(2S)-butan-2-yl]-8,11,20-trimethyl-3,6,9,21-tetraoxo-2-[(prop-2-enoylamino)methyl]-1,4,7,10-tetrazacyclohenicos-15-ene-11-carbonyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S,8S,11S,19S)-11-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]carbamoyl]-2-[(2S)-butan-2-yl]-8-(carboxymethyl)-3,6,9,13,20-pentaoxo-1,4,7,10,14-pentazacycloicos-19-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid	1715809: Binding affinity to human Bcl2A1 incubated for 2 hrs by FBid based competitive FP assay	ic50	0.0066	uM
(3S)-3-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2R)-2-acetamido-3-sulfanylpropanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]amino]-5-amino-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]-4-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1,4-diamino-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-oxobutanoic acid	1802502: DELFIA from Article 10.1021/acschembio.6b00962: “hBfl-1/hNOXA Interaction Studies Provide New Insights on the Role of Bfl-1 in Cancer Cell Resistance and for the Design of Novel Anticancer Agents.”	ic50	0.0075	uM
(4S)-4-[[(5S,8S,11S,15E,20S)-20-acetamido-5-[(2S)-butan-2-yl]-8,11,20-trimethyl-3,6,9,21-tetraoxo-2-[(prop-2-enoylamino)methyl]-1,4,7,10-tetrazacyclohenicos-15-ene-11-carbonyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(3S,9S,12S,16E,21S)-21-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]carbamoyl]-9-[(2S)-butan-2-yl]-3-(carboxymethyl)-12,21-dimethyl-2,5,8,11-tetraoxo-1,4,7,10-tetrazacyclohenicos-16-en-12-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid	1715809: Binding affinity to human Bcl2A1 incubated for 2 hrs by FBid based competitive FP assay	ic50	0.0134	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[2-[[(2S,3S)-2-acetamido-3-methylpentanoyl]amino]-3-(prop-2-enoylamino)propanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-5-amino-5-oxopentanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(3S,9S,12S,16E,21S)-21-[[(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]carbamoyl]-9-[(2S)-butan-2-yl]-3-(carboxymethyl)-12,21-dimethyl-2,5,8,11-tetraoxo-1,4,7,10-tetrazacyclohenicos-16-en-12-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid	1715809: Binding affinity to human Bcl2A1 incubated for 2 hrs by FBid based competitive FP assay	ic50	0.0135	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[2-acetamido-3-[(2-chloroacetyl)amino]propanoyl]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]-2-methyl-1-oxohept-6-en-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-2-methyl-1-oxohept-6-en-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid	1802502: DELFIA from Article 10.1021/acschembio.6b00962: “hBfl-1/hNOXA Interaction Studies Provide New Insights on the Role of Bfl-1 in Cancer Cell Resistance and for the Design of Novel Anticancer Agents.”	ic50	0.0139	uM
(3S)-3-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2R)-2-acetamido-3-sulfanylpropanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]amino]-5-amino-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]-4-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1,4-diamino-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-oxobutanoic acid	1802502: DELFIA from Article 10.1021/acschembio.6b00962: “hBfl-1/hNOXA Interaction Studies Provide New Insights on the Role of Bfl-1 in Cancer Cell Resistance and for the Design of Novel Anticancer Agents.”	ic50	0.0150	uM
(4S)-4-[[(2S)-5-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,3S)-2-amino-3-methylpentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-methylpentanoyl]amino]propanoyl]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)-5-carbamimidamido-1-[[(1S)-4-carbamimidamido-1-carboxybutyl]amino]-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	1831750: Inhibition of human Bfl-1 (1 to 149 residues) expressed in Rosetta-gami (DE3) using biotinylated-BH3 peptide as substrate measured after 2 hrs by DELFIA displacement assay	ic50	0.0180	uM
(4S)-4-[[(5S,8S,11S,19S)-19-acetamido-5-[(2S)-butan-2-yl]-8-methyl-3,6,9,13,20-pentaoxo-2-[(prop-2-enoylamino)methyl]-1,4,7,10,14-pentazacycloicosane-11-carbonyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(3S,9S,12S,16E,21S)-21-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]carbamoyl]-9-[(2S)-butan-2-yl]-3-(carboxymethyl)-12,21-dimethyl-2,5,8,11-tetraoxo-1,4,7,10-tetrazacyclohenicos-16-en-12-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid	1715809: Binding affinity to human Bcl2A1 incubated for 2 hrs by FBid based competitive FP assay	ic50	0.0204	uM
N-[4-[(1R,3R)-3-aminocyclopentyl]oxyphenyl]-N-[(1S)-1-[3-cyano-4-(trifluoromethyl)phenyl]ethyl]prop-2-enamide	2127449: Inhibition of N-terminal His6-tagged recombinant Bfl-1 (1 to 151 residues)(unknown origin) extracted from Escherichia coli BL21-Gold (DE3) using HyLite Fluor 647-labeled Bim peptide as substrate incubated for 120 mins by TR-FRET assay	ic50	0.0220	uM
(2S)-2-acetamido-N-[2-[2-(dimethylamino)ethyldisulfanyl]ethyl]-3-(1H-indol-3-yl)propanamide	1938337: Displacement of fluorescent-labeled BID-BH3 peptide from His-tagged BFL-1 (unknown origin)	ec50	0.0230	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	1715809: Binding affinity to human Bcl2A1 incubated for 2 hrs by FBid based competitive FP assay	ic50	0.0309	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-[[(3S,9S,12S,21S)-21-[[(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]carbamoyl]-9-[(2S)-butan-2-yl]-3-(carboxymethyl)-12,21-dimethyl-2,5,8,11-tetraoxo-1,4,7,10-tetrazacyclohenicos-16-en-12-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid	1337035: Inhibition of FITC-betaA-DIIRNIARHLAQVGDSMRSI-NH2 binding to recombinant human Bcl2A1 (1 to 152 residues) BH3 binding site expressed in Escherichia coli measured after 2 hrs by fluorescence polarization assay	ki	0.0320	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[2-[[(2S,3S)-2-acetamido-3-methylpentanoyl]amino]-3-(prop-2-enoylamino)propanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-5-amino-5-oxopentanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(3S,9S,12S,16E,21S)-21-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]carbamoyl]-9-[(2S)-butan-2-yl]-3-(carboxymethyl)-12,21-dimethyl-2,5,8,11-tetraoxo-1,4,7,10-tetrazacyclohenicos-16-en-12-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid	1715809: Binding affinity to human Bcl2A1 incubated for 2 hrs by FBid based competitive FP assay	ic50	0.0546	uM
N-[4-[(1R,3R)-3-aminocyclopentyl]oxyphenyl]-N-[(1S)-1-(4-chlorophenyl)ethyl]prop-2-enamide	2127449: Inhibition of N-terminal His6-tagged recombinant Bfl-1 (1 to 151 residues)(unknown origin) extracted from Escherichia coli BL21-Gold (DE3) using HyLite Fluor 647-labeled Bim peptide as substrate incubated for 120 mins by TR-FRET assay	ic50	0.0630	uM
(3S)-3-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-4-sulfanylbutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]amino]-5-amino-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]-4-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1,4-diamino-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-oxobutanoic acid	1802502: DELFIA from Article 10.1021/acschembio.6b00962: “hBfl-1/hNOXA Interaction Studies Provide New Insights on the Role of Bfl-1 in Cancer Cell Resistance and for the Design of Novel Anticancer Agents.”	ic50	0.0830	uM
2-[[4-(4-tert-butylphenyl)piperazin-1-yl]sulfonylamino]-5-(2-phenylethylsulfanyl)benzoic acid	1546924: Inhibition of N-terminal His6-tagged human Bfl-1 (1 to 151 residues), expressed in Escherichia coli Rosetta2 DE3 by fluorescent labeled FAM-Bid peptide based fluorescence polarization assay	ki	0.0840	uM
2-[[4-[(4-tert-butylphenyl)methyl]piperazin-1-yl]sulfonylamino]-5-(2-phenylethylsulfanyl)benzoic acid	1546924: Inhibition of N-terminal His6-tagged human Bfl-1 (1 to 151 residues), expressed in Escherichia coli Rosetta2 DE3 by fluorescent labeled FAM-Bid peptide based fluorescence polarization assay	ki	0.1000	uM
2-[[4-(4-tert-butylphenyl)piperazin-1-yl]sulfonylamino]-5-[2-(3-methoxyphenyl)ethylsulfanyl]benzoic acid	1546924: Inhibition of N-terminal His6-tagged human Bfl-1 (1 to 151 residues), expressed in Escherichia coli Rosetta2 DE3 by fluorescent labeled FAM-Bid peptide based fluorescence polarization assay	ki	0.1000	uM
4-[4-[[1-(4-chloro-2-ethylphenyl)-6-(prop-2-enoylamino)-3,4-dihydronaphthalen-2-yl]methyl]piperazin-1-yl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoic acid	2066213: Inhibition of BFL-1 (unknown origin)/ fluorescein-tagged Bid BH3 peptide (79 to 99) (unknown origin) interaction measured after 24 hrs incubation by fluorescence polarization assay	ki	0.1050	uM
4-[4-[[1-(4-chloro-2-ethylphenyl)-6-[ethyl(prop-2-enoyl)amino]-3,4-dihydronaphthalen-2-yl]methyl]piperazin-1-yl]benzoic acid	2066213: Inhibition of BFL-1 (unknown origin)/ fluorescein-tagged Bid BH3 peptide (79 to 99) (unknown origin) interaction measured after 24 hrs incubation by fluorescence polarization assay	ki	0.1100	uM
5-benzyl-2-(5-benzyl-1,4,6,7-tetrahydroxy-3-methylnaphthalen-2-yl)-3-methylnaphthalene-1,4,6,7-tetrone	1483470: Inhibition of FITC-labeled Bim BH3 binding to GST-tagged Bcl2A1 (unknown origin) preincubated for 2 mins followed by FITC-Bim-BH3 addition measured after 10 mins by fluorescence polarization assay	ic50	0.1220	uM
4-[4-[[1-(4-chloro-2-ethylphenyl)-6-[prop-2-enoyl(propyl)amino]-3,4-dihydronaphthalen-2-yl]methyl]piperazin-1-yl]benzoic acid	2066213: Inhibition of BFL-1 (unknown origin)/ fluorescein-tagged Bid BH3 peptide (79 to 99) (unknown origin) interaction measured after 24 hrs incubation by fluorescence polarization assay	ki	0.1240	uM
4-[4-[[1-(4-chlorophenyl)-6-(prop-2-enoylamino)-3,4-dihydronaphthalen-2-yl]methyl]piperazin-1-yl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoic acid	2066213: Inhibition of BFL-1 (unknown origin)/ fluorescein-tagged Bid BH3 peptide (79 to 99) (unknown origin) interaction measured after 24 hrs incubation by fluorescence polarization assay	ki	0.1270	uM
4-[4-[[1-(4-chloro-2-ethylphenyl)-6-[propan-2-yl(prop-2-enoyl)amino]-3,4-dihydronaphthalen-2-yl]methyl]piperazin-1-yl]benzoic acid	2066213: Inhibition of BFL-1 (unknown origin)/ fluorescein-tagged Bid BH3 peptide (79 to 99) (unknown origin) interaction measured after 24 hrs incubation by fluorescence polarization assay	ki	0.1400	uM
4-[4-[[1-(4-chlorophenyl)-6-(prop-2-enoylamino)-3,4-dihydronaphthalen-2-yl]methyl]piperazin-1-yl]-2-(1-methylpyrrolo[2,3-b]pyridin-5-yl)oxybenzoic acid	2066213: Inhibition of BFL-1 (unknown origin)/ fluorescein-tagged Bid BH3 peptide (79 to 99) (unknown origin) interaction measured after 24 hrs incubation by fluorescence polarization assay	ki	0.1450	uM
5-(2-phenylethylsulfanyl)-2-[(4-phenylphenyl)sulfonylamino]benzoic acid	1546924: Inhibition of N-terminal His6-tagged human Bfl-1 (1 to 151 residues), expressed in Escherichia coli Rosetta2 DE3 by fluorescent labeled FAM-Bid peptide based fluorescence polarization assay	ki	0.1500	uM
4-[4-[[1-(4-chloro-2-ethylphenyl)-6-(prop-2-enoylamino)-3,4-dihydronaphthalen-2-yl]methyl]piperazin-1-yl]benzoic acid	2066213: Inhibition of BFL-1 (unknown origin)/ fluorescein-tagged Bid BH3 peptide (79 to 99) (unknown origin) interaction measured after 24 hrs incubation by fluorescence polarization assay	ki	0.1580	uM
2-[(4-cyclohexylphenyl)sulfonylamino]-5-(2-phenylethylsulfanyl)benzoic acid	1546924: Inhibition of N-terminal His6-tagged human Bfl-1 (1 to 151 residues), expressed in Escherichia coli Rosetta2 DE3 by fluorescent labeled FAM-Bid peptide based fluorescence polarization assay	ki	0.1700	uM
(Z)-4-[(1S,2S,8R,17S,19R)-12-hydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoic acid	1984788: Inhibition of recombinant Bfl-1 (1-152) (unknown origin) by TR-FRET assay	ic50	0.1760	uM
4-[4-[[1-(4-chlorophenyl)-6-(prop-2-enoylamino)-3,4-dihydronaphthalen-2-yl]methyl]piperazin-1-yl]-2-phenylbenzoic acid	2066213: Inhibition of BFL-1 (unknown origin)/ fluorescein-tagged Bid BH3 peptide (79 to 99) (unknown origin) interaction measured after 24 hrs incubation by fluorescence polarization assay	ki	0.1780	uM
5-hydroxy-2,3,7-trimethyl-N-(2-phenylpropyl)-6-[1,6,7-trihydroxy-5-(2-phenylpropylcarbamoyl)naphthalen-2-yl]naphthalene-1-carboxamide	1858790: Inhibition of Bfl-1/Bak (unknown origin)	ic50	0.2000	uM
4-[4-[[1-(4-chloro-2-ethylphenyl)-6-[methyl(prop-2-enoyl)amino]-3,4-dihydronaphthalen-2-yl]methyl]piperazin-1-yl]benzoic acid	2066213: Inhibition of BFL-1 (unknown origin)/ fluorescein-tagged Bid BH3 peptide (79 to 99) (unknown origin) interaction measured after 24 hrs incubation by fluorescence polarization assay	ki	0.2180	uM
3-chloro-1-(3,4-dichlorophenyl)-4-[4-(2-hydroxyethyl)piperazin-1-yl]pyrrole-2,5-dione	528201: Inhibition of N-terminal FITC BH3 peptide binding to GST-tagged Bfl1 by fluorescence polarization assay	ic50	0.2400	uM
2-[[4-(4-tert-butylphenyl)piperazin-1-yl]sulfonylamino]-5-[2-(3-hydroxyphenyl)ethylsulfanyl]benzoic acid	1546924: Inhibition of N-terminal His6-tagged human Bfl-1 (1 to 151 residues), expressed in Escherichia coli Rosetta2 DE3 by fluorescent labeled FAM-Bid peptide based fluorescence polarization assay	ki	0.2500	uM
3-chloro-1-(3,4-dichlorophenyl)-4-[4-[(E)-3-phenylprop-2-enyl]piperazin-1-yl]pyrrole-2,5-dione	528201: Inhibition of N-terminal FITC BH3 peptide binding to GST-tagged Bfl1 by fluorescence polarization assay	ic50	0.2500	uM
4-[4-[[1-(4-chloro-2-methylphenyl)-6-(prop-2-enoylamino)-3,4-dihydronaphthalen-2-yl]methyl]piperazin-1-yl]benzoic acid	2066213: Inhibition of BFL-1 (unknown origin)/ fluorescein-tagged Bid BH3 peptide (79 to 99) (unknown origin) interaction measured after 24 hrs incubation by fluorescence polarization assay	ki	0.2510	uM
4-[4-[[1-(2,4-dichlorophenyl)-6-(prop-2-enoylamino)-3,4-dihydronaphthalen-2-yl]methyl]piperazin-1-yl]benzoic acid	2066213: Inhibition of BFL-1 (unknown origin)/ fluorescein-tagged Bid BH3 peptide (79 to 99) (unknown origin) interaction measured after 24 hrs incubation by fluorescence polarization assay	ki	0.2560	uM
1-[4-[2-benzyl-6-(3-fluorophenyl)indazol-3-yl]piperazin-1-yl]prop-2-en-1-one	1907206: Binding affinity to His-tagged recombinant BFL-1 (1 to 151 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by surface plasmon resonance analysis	kd	0.2624	uM
4-[(E)-(4-methyl-2-phenylimino-1,3-thiazol-3-yl)iminomethyl]benzene-1,2,3-triol;hydrochloride	1938336: Inhibition of Bfl-1 (unknown origin) by fluorescence polarization assay	ic50	0.2640	uM
5-(2-phenylethylsulfanyl)-2-[(6-phenyl-3-pyridinyl)sulfonylamino]benzoic acid	1546924: Inhibition of N-terminal His6-tagged human Bfl-1 (1 to 151 residues), expressed in Escherichia coli Rosetta2 DE3 by fluorescent labeled FAM-Bid peptide based fluorescence polarization assay	ki	0.2800	uM
(3S)-3-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[2-acetamido-3-[(2-chloroacetyl)amino]propanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]amino]-5-amino-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]-4-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1,4-diamino-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-oxobutanoic acid	1802502: DELFIA from Article 10.1021/acschembio.6b00962: “hBfl-1/hNOXA Interaction Studies Provide New Insights on the Role of Bfl-1 in Cancer Cell Resistance and for the Design of Novel Anticancer Agents.”	ic50	0.2870	uM
3-chloro-1-(3,4-dichlorophenyl)-4-[4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl]pyrrole-2,5-dione	528201: Inhibition of N-terminal FITC BH3 peptide binding to GST-tagged Bfl1 by fluorescence polarization assay	ic50	0.3000	uM
N-[4-[(1R,3R)-3-aminocyclopentyl]oxyphenyl]-N-[[3-cyano-4-(trifluoromethyl)phenyl]methyl]prop-2-enamide	2127449: Inhibition of N-terminal His6-tagged recombinant Bfl-1 (1 to 151 residues)(unknown origin) extracted from Escherichia coli BL21-Gold (DE3) using HyLite Fluor 647-labeled Bim peptide as substrate incubated for 120 mins by TR-FRET assay	ic50	0.3000	uM
3-chloro-1-(3,4-dichlorophenyl)-4-(dimethylamino)pyrrole-2,5-dione	528201: Inhibition of N-terminal FITC BH3 peptide binding to GST-tagged Bfl1 by fluorescence polarization assay	ic50	0.3000	uM
4-[4-[[1-(4-chlorophenyl)-6-[[methyl(prop-2-enoyl)amino]methyl]-3,4-dihydronaphthalen-2-yl]methyl]piperazin-1-yl]benzoic acid	2066213: Inhibition of BFL-1 (unknown origin)/ fluorescein-tagged Bid BH3 peptide (79 to 99) (unknown origin) interaction measured after 24 hrs incubation by fluorescence polarization assay	ki	0.3260	uM
4-[4-[[1-(4-chlorophenyl)-6-[[ethyl(prop-2-enoyl)amino]methyl]-3,4-dihydronaphthalen-2-yl]methyl]piperazin-1-yl]benzoic acid	2066213: Inhibition of BFL-1 (unknown origin)/ fluorescein-tagged Bid BH3 peptide (79 to 99) (unknown origin) interaction measured after 24 hrs incubation by fluorescence polarization assay	ki	0.3350	uM
N-[4-[(1R,3R)-3-aminocyclopentyl]oxyphenyl]-N-[(4-chlorophenyl)methyl]prop-2-enamide	2127449: Inhibition of N-terminal His6-tagged recombinant Bfl-1 (1 to 151 residues)(unknown origin) extracted from Escherichia coli BL21-Gold (DE3) using HyLite Fluor 647-labeled Bim peptide as substrate incubated for 120 mins by TR-FRET assay	ic50	0.3400	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Tretinoin	affects cotreatment, increases expression, decreases response to substance	6
Arsenic Trioxide	decreases expression, increases expression, affects cotreatment	5
Benzo(a)pyrene	increases methylation, affects methylation, decreases expression, increases expression	5
Silicon Dioxide	increases expression	5
Methotrexate	decreases response to substance, affects cotreatment, decreases expression, increases expression	4
(+)-JQ1 compound	decreases expression	3
Cisplatin	increases expression	3
Doxorubicin	affects response to substance, decreases expression, decreases response to substance, increases expression	3
Lipopolysaccharides	increases expression, affects response to substance	3
Paraquat	affects cotreatment, increases expression, decreases expression	3
Tetradecanoylphorbol Acetate	decreases reaction, increases expression, affects cotreatment, affects expression	3
Antirheumatic Agents	affects cotreatment, decreases response to substance, decreases expression	3
bisphenol A	increases expression, affects cotreatment	2
sodium arsenite	increases expression	2
Resveratrol	decreases expression, increases expression	2
Calcitriol	increases expression	2
Curcumin	decreases reaction, increases expression, decreases expression	2
Nickel	increases expression	2
Toluene	increases expression	2
Aflatoxin B1	increases expression, increases methylation	2
Cadmium Chloride	decreases expression	2
aristolochic acid I	increases expression	1
moringin	affects cotreatment, increases expression	1
aminomethylphosphonic acid (AMPA)	increases expression	1
ethylbenzene	increases expression	1
naringenin	affects cotreatment, increases expression	1
triphenyl phosphate	affects expression	1
propionaldehyde	increases expression	1
bis(tri-n-butyltin)oxide	increases expression	1
kaempferol	decreases reaction, increases expression	1

ChEMBL screening assays

154 unique, capped per target: 152 binding, 2 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1251056	Binding	Inhibition of GST-tagged Bfl-1/FITC-conjugated Bax interaction by fluorescence polarisation assay	Synthesis and biological activities of new di- and trimeric quinoline derivatives. — Bioorg Med Chem
CHEMBL1794562	Functional	PUBCHEM_BIOASSAY: Secondary assay of A1 inhibitors in Mouse Embryonic Fibroblasts with alternate A1 construct Measured in Cell-Based System Using Plate Reader - 2045-05_Inhibitor_Dose_DryPowder_Activity_Set2. (Class of assay: confirmatory)	PubChem BioAssay data set

Cellosaurus cell lines

1 cell lines: 1 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_D7KW	Ubigene A-549 BCL2A1 KO	Cancer cell line	Male

Clinical trials (associated diseases)

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