BIRC2

Summary

BIRC2 (baculoviral IAP repeat containing 2, HGNC:590) is a protein-coding gene on chromosome 11q22.2, encoding Baculoviral IAP repeat-containing protein 2 (Q13490). Multi-functional protein which regulates not only caspases and apoptosis, but also modulates inflammatory signaling and immunity, mitogenic kinase signaling, and cell proliferation, as well as cell invasion and metastasis. It is a selective cancer dependency (DepMap: 12.0% of cell lines).

The protein encoded by this gene is a member of a family of proteins that inhibits apoptosis by binding to tumor necrosis factor receptor-associated factors TRAF1 and TRAF2, probably by interfering with activation of ICE-like proteases. This encoded protein inhibits apoptosis induced by serum deprivation and menadione, a potent inducer of free radicals. Alternatively spliced transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 329 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 100 total
• Druggable target: yes — 5 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 12.0% of screened cell lines
• MANE Select transcript: NM_001166

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:590
Approved symbol	BIRC2
Name	baculoviral IAP repeat containing 2
Location	11q22.2
Locus type	gene with protein product
Status	Approved
Aliases	cIAP1, hiap-2, MIHB, RNF48, c-IAP1
Ensembl gene	ENSG00000110330
Ensembl biotype	protein_coding
OMIM	601712
Entrez	329

Gene structure

Transcript identifiers

Ensembl transcripts: 22 — 17 protein_coding, 3 protein_coding_CDS_not_defined, 1 nonsense_mediated_decay, 1 retained_intron

ENST00000227758, ENST00000527465, ENST00000527808, ENST00000527910, ENST00000528344, ENST00000530675, ENST00000531259, ENST00000532672, ENST00000532832, ENST00000533742, ENST00000534130, ENST00000534646, ENST00000613397, ENST00000866596, ENST00000866597, ENST00000866598, ENST00000866599, ENST00000866600, ENST00000866601, ENST00000922854, ENST00000922855, ENST00000948252

RefSeq mRNA: 3 — MANE Select: NM_001166 NM_001166, NM_001256163, NM_001256166

CCDS: CCDS58169, CCDS8316

Canonical transcript exons

ENST00000227758 — 9 exons

Exon	Start	End
ENSE00002181047	102347214	102347376
ENSE00003466586	102363668	102363716
ENSE00003504775	102362896	102362974
ENSE00003519792	102377857	102377898
ENSE00003590111	102377496	102377750
ENSE00003598444	102348598	102350749
ENSE00003600416	102350844	102350943
ENSE00003612642	102368306	102368548
ENSE00003617386	102377990	102378670

Expression profiles

Bgee: expression breadth ubiquitous, 299 present calls, max score 99.28.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 58.1938 / max 699.0799, expressed in 1823 samples.

FANTOM5 promoters (9 alternative TSS)

Promoter ID	TPM avg	Samples expressed
116414	54.5794	1820
116410	1.2404	465
116416	0.7837	382
116415	0.4897	201
116418	0.4827	203
116413	0.2334	83
116412	0.1597	47
116411	0.1580	52
116409	0.0669	18

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
cartilage tissue	UBERON:0002418	99.28	gold quality
secondary oocyte	CL:0000655	99.13	gold quality
endothelial cell	CL:0000115	98.47	gold quality
oocyte	CL:0000023	98.31	gold quality
epithelium of nasopharynx	UBERON:0001951	97.90	gold quality
germinal epithelium of ovary	UBERON:0001304	97.78	gold quality
tibia	UBERON:0000979	97.59	gold quality
visceral pleura	UBERON:0002401	97.52	gold quality
pleura	UBERON:0000977	97.45	gold quality
parietal pleura	UBERON:0002400	97.45	gold quality
pancreatic ductal cell	CL:0002079	97.23	gold quality
ventricular zone	UBERON:0003053	97.11	gold quality
corpus epididymis	UBERON:0004359	97.01	gold quality
mucosa of urinary bladder	UBERON:0001259	96.98	gold quality
trigeminal ganglion	UBERON:0001675	96.83	gold quality
palpebral conjunctiva	UBERON:0001812	96.69	gold quality
cervix squamous epithelium	UBERON:0006922	96.68	gold quality
mucosa of paranasal sinus	UBERON:0005030	96.66	gold quality
adrenal tissue	UBERON:0018303	96.56	gold quality
periodontal ligament	UBERON:0008266	96.52	gold quality
nephron tubule	UBERON:0001231	96.45	gold quality
trabecular bone tissue	UBERON:0002483	96.38	gold quality
renal glomerulus	UBERON:0000074	96.32	gold quality
metanephric glomerulus	UBERON:0004736	96.28	gold quality
bronchial epithelial cell	CL:0002328	96.25	gold quality
mucosa of sigmoid colon	UBERON:0004993	96.24	gold quality
colonic mucosa	UBERON:0000317	96.14	gold quality
calcaneal tendon	UBERON:0003701	96.14	gold quality
corpus callosum	UBERON:0002336	96.12	gold quality
dorsal root ganglion	UBERON:0000044	96.11	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	6.05

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): ETS1, FOXA2, KAT5, NFKB1, NFKB, REL, RELA, STAT1

miRNA regulators (miRDB)

41 targeting BIRC2, 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-29A-3P	100.00	73.11	1835
HSA-MIR-29B-3P	100.00	73.18	1833
HSA-MIR-29C-3P	100.00	73.15	1833
HSA-MIR-6870-5P	99.99	68.55	2115
HSA-MIR-4723-5P	99.97	68.70	2034
HSA-MIR-5698	99.97	68.49	2029
HSA-MIR-7111-5P	99.97	68.48	2062
HSA-MIR-3065-5P	99.97	71.56	3281
HSA-MIR-1229-3P	99.97	66.49	906
HSA-MIR-767-5P	99.95	70.85	993
HSA-MIR-6835-3P	99.93	70.49	2904
HSA-MIR-145-5P	99.92	71.13	1836
HSA-MIR-5195-3P	99.92	70.92	1877
HSA-MIR-498-3P	99.91	71.27	1114
HSA-MIR-627-3P	99.90	71.42	3316
HSA-MIR-204-5P	99.79	71.62	2439
HSA-MIR-211-5P	99.79	71.65	2440
HSA-MIR-623	99.76	68.16	1170
HSA-MIR-6794-5P	99.76	66.38	1048
HSA-MIR-4766-5P	99.75	69.23	2662
HSA-MIR-4255	99.72	67.70	1541
HSA-MIR-4755-5P	99.71	70.34	2716
HSA-MIR-5006-3P	99.71	70.26	2728
HSA-MIR-4716-3P	99.69	66.73	1022
HSA-MIR-3175	99.65	66.30	2031
HSA-MIR-7159-5P	99.53	72.12	2472
HSA-MIR-6832-3P	99.52	70.44	1726
HSA-MIR-657	99.48	66.02	848
HSA-MIR-32-3P	99.36	68.20	2517
HSA-MIR-6780B-3P	99.13	67.18	622

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 12.0% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 40)

• Expression of cIAP1, a target for 11q22 amplification, correlates with resistance of cervical cancers to radiotherapy. (PMID:12208731)
• CD40 engagement enhances eosinophil survival through induction of cellular inhibitor of apoptosis protein 2 expression: implications for allergic inflammation (PMID:12209092)
• Smac-penetratin fusion peptide crossed the cellular membrane, bound XIAP and cIAP1, displaced caspase-3 from cytoplasmic aggregates, and enhanced drug-induced caspase action in situ (PMID:12218061)
• These results indicate that IAPs alone are not the main factor responsible for the resistance of non-small-cell lung cancer cells to treatment. (PMID:12243753)
• Reovirus-induced apoptosis involves reduction of cellular IAP1 protein levels (PMID:12388702)
• Cellular inhibitors of apoptosis 1 and 2 are ubiquitin ligases for the apoptosis inducer Smac/DIABLO. (PMID:12525502)
• TRAF2, TRAF3, cIAP1, Smac, and lymphotoxin beta receptor associate and are involved in apoptosis (PMID:12571250)
• c-IAP1 is an important intracellular modulator of Fas- as well as TNF-alpha death signalling pathways in human vascular smooth muscle cells. (PMID:12603340)
• cIAP1 and cIAP2 are potential oncogenes and are overexpressed in multiple lung cancers with or without higher copy numbers (PMID:12651874)
• although cIAP-1, cIAP-2 and XIAP transcripts were highly upregulated, their expression of endogenous proteins were not increased in HUVECs stimulated with LPS (PMID:12851723)
• cIAP-1 has a role in regulating cell survival in endometrial cancer cells (PMID:12888921)
• Relative risk of death was lower for cytoplasmic c-IAP1, cytoplasmic c-IAP2, and nuclear c-IAP2 expression. It was higher for nuclear c-IAP1 expression. (PMID:14708638)
• levels of c-IAP1 and c-IAP2 are regulated by Smac/DIABLO through the ubiquitin/proteasome pathway (PMID:14960576)
• HIAP2 is translationally induced during endoplasmic reticulum stress (PMID:14960583)
• X-linked XIAP is present in Chronic lymphocytic leukemia cells and is up-regulated in conditions where apoptosis is prevented. (PMID:15183896)
• c-IAP1 cellular location has a role in regulating cell differentiation (PMID:15187025)
• No association of the TAP2 gene with schizophrenia in the Korean population. (PMID:15318034)
• CIAP1 is downregulated and/or cleaved in a dose-dependent manner upon by anti-cancer drugs. cIAP-1’s mitochondrial localization & liberation indicate a profoundly different function of this protein despite its similar modular structure to XIAP. (PMID:15359644)
• expression in urethral epithelium upregulated by Neisseria gonorrhoeae PorB IB and upregulation dependent on NF-kappaB activation (PMID:15501771)
• role for overexpressed cIAP1 in genetic instability, possibly by interfering with mitotic functions (PMID:15665297)
• nuclear cIAP-1 expression appears to be a useful marker for predicting poor prognosis in head and neck squamous cell carcinoma (HNSCC), and may play roles in HNSCCs through the signaling pathway mediated by Smac/DIABLO and caspase-3 (PMID:15911110)
• There is endogenous cLAP1 expression in MKN45 cells, which may be a factor in the presumed anti-apoptotic system in these human gastric cancer cells. (PMID:16080516)
• IAP1 protects neural progenitor cells against TRAIL-induced apoptosis and suppresses caspase-3 activation. (PMID:16180223)
• a single cIAP can direct its E3 ligase activity toward different substrates and can alter the cellular functions of different protein targets, including TRAF2 and SMAC, in accordance with differences in the specificity of individual BIR domains (PMID:16282325)
• cIAP1 and cIAP2 bind but do not inhibit caspases (PMID:16339151)
• Since F-box proteins are specificity determining subunits of SCF ubiquitin protein ligases, our results suggest that Fbxo7 can mediate the ubiquitination of cIAP1 by SCF ubiquitin protein ligase and in the regulation of cIAP1 function. (PMID:16510124)
• Results indicate a novel mechanism by which HIAP2 can regulate ER-initiated apoptosis by modulating the activity of caspase-2. (PMID:16701639)
• High cIAP membranous expression is associated with epithelial ovarian cancer (PMID:16775178)
• IAP family proteins may the prognosis of multiple myeloma patients in association with chemotherapy-induced overexpression of MDR1 or LRP. (PMID:16929535)
• Differential expression of IAPs in B-cell lymphomas suggests differences in pathogenesis that may have implications for novel treatment strategies targeting IAPs. (PMID:16983704)
• TNFR2 signaling induces selective c-IAP1-dependent ASK1 ubiquitination and terminates mitogen-activated protein kinase signaling (PMID:17220297)
• Bortezomib inhibited expression of cIAP-1, cIAP-2, and XIAP, which are regulated by NF-kappaB and function as inhibitors of apoptosis. (PMID:17626072)
• Importantly, our findings suggest that a paradox exists whereby Nrf2 activity is beneficial in non-malignant cells but in cancer cells it may provide a selective advantage for clonal expansion. (PMID:17822677)
• Data show that Cartilage oligomeric matrix protein protects cells against death by elevating cIAP1 proteins. (PMID:17993464)
• ME-BS directly interacts with the BIR3 domain of cIAP1, promotes auto-ubiquitylation dependent on its RING domain, and facilitates proteasomal degradation of cIAP1. (PMID:18230607)
• Results suggest that HSP90 beta prevents auto-ubiquitination and degradation of its client protein c-IAP1, whose depletion would be sufficient to inhibit cell differentiation. (PMID:18239673)
• the RING domain of cIAP1 mediates the degradation of RING-bearing inhibitor of apoptosis proteins by distinct pathways (PMID:18434593)
• HIAP-1 and HIAP-2 mRNA levels were elevated in resting T cells while NAIP mRNA was increased in whole blood in multiple sclerosis (PMID:18566024)
• cIAP1 and cIAP2 promote cancer cell survival by functioning as E3 ubiquitin ligases that maintain constitutive ubiquitination of the RIP1 adaptor protein. (PMID:18570872)
• Nuclear, cytoplasmic and concurrent cIAP-1 immunoreactions were significantly correlated with lymph node metastasis in tongue squamous cell carcinomas. (PMID:18621506)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	birc2	ENSDARG00000044619
mus_musculus	Birc2	ENSMUSG00000057367
rattus_norvegicus	Birc2	ENSRNOG00000010602
drosophila_melanogaster	Diap2	FBGN0015247
caenorhabditis_elegans		WBGENE00000250

Paralogs (7): BIRC3 (ENSG00000023445), BIRC5 (ENSG00000089685), NLRC4 (ENSG00000091106), BIRC7 (ENSG00000101197), XIAP (ENSG00000101966), BIRC6 (ENSG00000115760), NAIP (ENSG00000249437)

Protein

Protein identifiers

Baculoviral IAP repeat-containing protein 2 — Q13490 (reviewed: Q13490)

Alternative names: Cellular inhibitor of apoptosis 1, IAP homolog B, Inhibitor of apoptosis protein 2, RING finger protein 48, RING-type E3 ubiquitin transferase BIRC2, TNFR2-TRAF-signaling complex protein 2

All UniProt accessions (7): Q13490, E9PI77, E9PIW1, E9PMH5, E9PNM6, E9PQZ9, H0YDY3

UniProt curated annotations — full annotation on UniProt →

Function. Multi-functional protein which regulates not only caspases and apoptosis, but also modulates inflammatory signaling and immunity, mitogenic kinase signaling, and cell proliferation, as well as cell invasion and metastasis. Acts as an E3 ubiquitin-protein ligase regulating NF-kappa-B signaling and regulates both canonical and non-canonical NF-kappa-B signaling by acting in opposite directions: acts as a positive regulator of the canonical pathway and suppresses constitutive activation of non-canonical NF-kappa-B signaling. The target proteins for its E3 ubiquitin-protein ligase activity include: RIPK1, RIPK2, RIPK3, RIPK4, CASP3, CASP7, CASP8, TRAF2, DIABLO/SMAC, MAP3K14/NIK, MAP3K5/ASK1, IKBKG/NEMO, IKBKE and MXD1/MAD1. Can also function as an E3 ubiquitin-protein ligase of the NEDD8 conjugation pathway, targeting effector caspases for neddylation and inactivation. Acts as an important regulator of innate immune signaling via regulation of Toll-like receptors (TLRs), Nodlike receptors (NLRs) and RIG-I like receptors (RLRs), collectively referred to as pattern recognition receptors (PRRs). Protects cells from spontaneous formation of the ripoptosome, a large multi-protein complex that has the capability to kill cancer cells in a caspase-dependent and caspase-independent manner. Suppresses ripoptosome formation by ubiquitinating RIPK1 and CASP8. Can stimulate the transcriptional activity of E2F1. Plays a role in the modulation of the cell cycle.

Subunit / interactions. Interacts with DIABLO/SMAC and with PRSS25; these interactions inhibit apoptotic suppressor activity. Interacts with CASP9. Interacts (via BIR domains) with TRAF2; the interaction is required for IKBKE ubiquitination. Interacts with E2F1, RIPK1, RIPK2, RIPK3, RIPK4, BIRC5/survivin and USP19. HSP90AB1. Interacts with UBXN1. Interacts with GSK3B. Interacts with several death receptors, inclusing FAS, TNFRSF10A and TNFRSF10B. Recruited to TNFRSF10B in the absence of receptor stimulation. When TNFRSF10B is stimulated, further recruited to the receptor and cleaved by caspases. Proteolytic fragments remain associated with TNFRSF10B.

Subcellular location. Cytoplasm. Nucleus.

Tissue specificity. Present in many fetal and adult tissues. Mainly expressed in adult skeletal muscle, thymus, testis, ovary, and pancreas, low or absent in brain and peripheral blood leukocytes.

Post-translational modifications. Auto-ubiquitinated and degraded by the proteasome in apoptotic cells. Upon stimulation of death receptors, including TNFRSF10B, recruited to receptors and cleaved by caspases. Proteolytic fragments remain associated with the receptors. This cleavage presumably inactivates the protein.

Activity regulation. The CARD domain inhibits the activation of E3 ubiquitin ligase activity by preventing RING domain dimerization and E2 ubiquitin donor binding and activation. The CARD domain-mediated autoinhibition of the E3 ubiquitin-protein ligase activity suppresses cell proliferation and migration. USP19 regulates the stability of BIRC2/c-IAP1 by preventing its ubiquitination.

Domain organisation. The BIR domains mediate nuclear localization. The CARD domain is necessary to stabilize the protein and inhibit the activation of E3 ubiquitin-protein ligase activity of BIRC2/c-IAP1 by preventing RING domain dimerization and E2 ubiquitin donor binding and activation.

Similarity. Belongs to the IAP family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q13490-1	1	yes
Q13490-2	2

RefSeq proteins (3): NP_001157, NP_001243092, NP_001243095 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001315	CARD	Domain
IPR001370	BIR_rpt	Repeat
IPR001841	Znf_RING	Domain
IPR011029	DEATH-like_dom_sf	Homologous_superfamily
IPR041933	BIRC2/BIRC3_UBA	Domain
IPR048875	BIRC2-3-like_UBA	Domain
IPR050784	IAP	Family

Pfam: PF00619, PF00653, PF13920, PF21290

UniProt features (72 total): helix 30, strand 15, turn 8, sequence variant 4, sequence conflict 4, binding site 4, repeat 3, chain 1, splice variant 1, domain 1, zinc finger region 1

Structure

Experimental structures (PDB)

29 structures.

PDB	Method	Resolution (Å)
4HY4	X-RAY DIFFRACTION	1.25
7QGJ	X-RAY DIFFRACTION	1.3
3D9T	X-RAY DIFFRACTION	1.5
8DSF	X-RAY DIFFRACTION	1.5
4KMN	X-RAY DIFFRACTION	1.52
4LGE	X-RAY DIFFRACTION	1.55
6HPR	X-RAY DIFFRACTION	1.7
7TRL	X-RAY DIFFRACTION	1.74
4HY5	X-RAY DIFFRACTION	1.75
3UW4	X-RAY DIFFRACTION	1.79
4MU7	X-RAY DIFFRACTION	1.79
5M6N	X-RAY DIFFRACTION	1.8
9N23	X-RAY DIFFRACTION	1.8
3T6P	X-RAY DIFFRACTION	1.9
3M1D	X-RAY DIFFRACTION	2
4LGU	X-RAY DIFFRACTION	2
6W74	X-RAY DIFFRACTION	2.11
4MTI	X-RAY DIFFRACTION	2.15
6W7O	X-RAY DIFFRACTION	2.17
6EXW	X-RAY DIFFRACTION	2.2
3D9U	X-RAY DIFFRACTION	2.3
8DSO	X-RAY DIFFRACTION	2.33
7TRM	X-RAY DIFFRACTION	2.4
3MUP	X-RAY DIFFRACTION	2.6
4EB9	X-RAY DIFFRACTION	2.6
3OZ1	X-RAY DIFFRACTION	3
6W8I	X-RAY DIFFRACTION	3.8
1QBH	SOLUTION NMR
2L9M	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q13490-F1	77.08	0.40

Functional residue map

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

Ligand- & substrate-binding residues (4): 306; 309; 326; 333

Function

Pathways and Gene Ontology

Reactome pathways

32 pathways

ID	Pathway
R-HSA-111465	Apoptotic cleavage of cellular proteins
R-HSA-168638	NOD1/2 Signaling Pathway
R-HSA-168927	TICAM1, RIP1-mediated IKK complex recruitment
R-HSA-5213460	RIPK1-mediated regulated necrosis
R-HSA-5357786	TNFR1-induced proapoptotic signaling
R-HSA-5357905	Regulation of TNFR1 signaling
R-HSA-5357956	TNFR1-induced NF-kappa-B signaling pathway
R-HSA-5668541	TNFR2 non-canonical NF-kB pathway
R-HSA-5675482	Regulation of necroptotic cell death
R-HSA-5676594	TNF receptor superfamily (TNFSF) members mediating non-canonical NF-kB pathway
R-HSA-5689880	Ub-specific processing proteases
R-HSA-937041	IKK complex recruitment mediated by RIP1
R-HSA-9958825	Activation of STAT3 by cadherin engagement
R-HSA-109581	Apoptosis
R-HSA-1280215	Cytokine Signaling in Immune system
R-HSA-162582	Signal Transduction
R-HSA-166016	Toll Like Receptor 4 (TLR4) Cascade
R-HSA-166166	MyD88-independent TLR4 cascade
R-HSA-168164	Toll Like Receptor 3 (TLR3) Cascade
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-168898	Toll-like Receptor Cascades
R-HSA-392499	Metabolism of proteins
R-HSA-5218859	Regulated Necrosis
R-HSA-5357801	Programmed Cell Death
R-HSA-5688426	Deubiquitination
R-HSA-597592	Post-translational protein modification
R-HSA-73887	Death Receptor Signaling
R-HSA-75153	Apoptotic execution phase

MSigDB gene sets: 374 (showing top): REACTOME_IKK_COMPLEX_RECRUITMENT_MEDIATED_BY_RIP1, GOBP_NEGATIVE_REGULATION_OF_PROTEIN_CONTAINING_COMPLEX_ASSEMBLY, WU_APOPTOSIS_BY_CDKN1A_VIA_TP53, MODULE_52, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_RESPONSE_TO_ETHANOL, REACTOME_INNATE_IMMUNE_SYSTEM, REACTOME_NOD1_2_SIGNALING_PATHWAY, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, GOBP_INFLAMMATORY_RESPONSE, GOBP_RESPONSE_TO_PEPTIDE, REACTOME_NUCLEOTIDE_BINDING_DOMAIN_LEUCINE_RICH_REPEAT_CONTAINING_RECEPTOR_NLR_SIGNALING_PATHWAYS, chr11q22, GOBP_NUCLEOTIDE_BINDING_DOMAIN_LEUCINE_RICH_REPEAT_CONTAINING_RECEPTOR_SIGNALING_PATHWAY, GOBP_CANONICAL_NF_KAPPAB_SIGNAL_TRANSDUCTION

GO Biological Process (38): protein polyubiquitination (GO:0000209), response to hypoxia (GO:0001666), placenta development (GO:0001890), apoptotic process (GO:0006915), cell surface receptor signaling pathway (GO:0007166), canonical NF-kappaB signal transduction (GO:0007249), positive regulation of protein ubiquitination (GO:0031398), tumor necrosis factor-mediated signaling pathway (GO:0033209), regulation of toll-like receptor signaling pathway (GO:0034121), non-canonical NF-kappaB signal transduction (GO:0038061), regulation of RIG-I signaling pathway (GO:0039535), regulation of cell population proliferation (GO:0042127), regulation of apoptotic process (GO:0042981), negative regulation of apoptotic process (GO:0043066), positive regulation of canonical NF-kappaB signal transduction (GO:0043123), negative regulation of canonical NF-kappaB signal transduction (GO:0043124), proteasome-mediated ubiquitin-dependent protein catabolic process (GO:0043161), regulation of innate immune response (GO:0045088), response to ethanol (GO:0045471), regulation of cell differentiation (GO:0045595), regulation of inflammatory response (GO:0050727), response to cAMP (GO:0051591), regulation of cell cycle (GO:0051726), regulation of necroptotic process (GO:0060544), negative regulation of necroptotic process (GO:0060546), necroptotic process (GO:0070266), regulation of nucleotide-binding domain, leucine rich repeat containing receptor signaling pathway (GO:0070424), regulation of non-canonical NF-kappaB signal transduction (GO:1901222), negative regulation of ripoptosome assembly involved in necroptotic process (GO:1902443), positive regulation of protein K63-linked ubiquitination (GO:1902523), positive regulation of protein K48-linked ubiquitination (GO:1902524), positive regulation of protein monoubiquitination (GO:1902527), response to bleomycin (GO:1904975), regulation of reactive oxygen species metabolic process (GO:2000377), positive regulation of DNA-templated transcription (GO:0045893), cellular response to tumor necrosis factor (GO:0071356), regulation of intracellular signal transduction (GO:1902531), positive regulation of protein polyubiquitination (GO:1902916)

GO Molecular Function (13): transcription coactivator activity (GO:0003713), ubiquitin-protein transferase activity (GO:0004842), zinc ion binding (GO:0008270), transferase activity (GO:0016740), identical protein binding (GO:0042802), cysteine-type endopeptidase inhibitor activity involved in apoptotic process (GO:0043027), ubiquitin binding (GO:0043130), protein-containing complex binding (GO:0044877), protein-folding chaperone binding (GO:0051087), ubiquitin protein ligase activity (GO:0061630), FBXO family protein binding (GO:0098770), protein binding (GO:0005515), metal ion binding (GO:0046872)

GO Cellular Component (7): XY body (GO:0001741), nucleus (GO:0005634), cytoplasm (GO:0005737), cytosol (GO:0005829), cytoplasmic side of plasma membrane (GO:0009898), CD40 receptor complex (GO:0035631), protein-containing complex (GO:0032991)

Reactome top-level categories

Rollup of top-15 pathways:

Category	Pathways
TNF signaling	3
Immune System	2
Toll-like Receptor Cascades	2
Apoptotic execution phase	1
Nucleotide-binding domain, leucine rich repeat containing receptor (NLR) signaling pathways	1
Toll Like Receptor 3 (TLR3) Cascade	1
Regulated Necrosis	1
Cytokine Signaling in Immune system	1
RIPK1-mediated regulated necrosis	1
TNFR2 non-canonical NF-kB pathway	1
Deubiquitination	1
TRIF (TICAM1)-mediated TLR4 signaling	1
Adherens junctions interactions	1
Programmed Cell Death	1
Toll Like Receptor 4 (TLR4) Cascade	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
protein binding	3
protein ubiquitination	2
intracellular signaling cassette	2
regulation of cellular process	2
apoptotic process	2
canonical NF-kappaB signal transduction	2
regulation of canonical NF-kappaB signal transduction	2
binding	2
cellular anatomical structure	2
response to stress	1
response to decreased oxygen levels	1
animal organ development	1
programmed cell death	1
apoptotic signaling pathway	1
execution phase of apoptosis	1
signal transduction	1
regulation of protein ubiquitination	1
positive regulation of protein modification by small protein conjugation or removal	1
cytokine-mediated signaling pathway	1
cellular response to tumor necrosis factor	1
toll-like receptor signaling pathway	1
regulation of pattern recognition receptor signaling pathway	1
RIG-I signaling pathway	1
regulation of cytoplasmic pattern recognition receptor signaling pathway	1
cell population proliferation	1
regulation of programmed cell death	1
regulation of apoptotic process	1
negative regulation of programmed cell death	1
positive regulation of intracellular signal transduction	1
negative regulation of intracellular signal transduction	1
ubiquitin-dependent protein catabolic process	1
proteasomal protein catabolic process	1
regulation of response to biotic stimulus	1
regulation of defense response	1
regulation of response to external stimulus	1
innate immune response	1
regulation of immune response	1
response to alcohol	1
cell differentiation	1
regulation of developmental process	1

Protein interactions and networks

STRING

2998 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
BIRC2	TRAF3	Q13114	998
BIRC2	TRAF1	Q13077	997
BIRC2	DIABLO	Q9NR28	997
BIRC2	RIPK1	Q13546	996
BIRC2	UBE2N	P61088	996
BIRC2	TRADD	Q15628	996
BIRC2	TNFRSF1A	P19438	995
BIRC2	TRAF2	Q12933	993
BIRC2	TRAF5	O00463	991
BIRC2	TRAF6	Q9Y4K3	974
BIRC2	BIRC3	Q13489	952
BIRC2	FADD	Q13158	941
BIRC2	CFLAR	O15519	938
BIRC2	IKBKG	Q9Y6K9	926
BIRC2	CASP9	P55211	911

IntAct

356 interactions, top by confidence:

A	B	Type	Score
TNF	TNFRSF1A	psi-mi:“MI:0914”(association)	0.960
TRAF2	BIRC2	psi-mi:“MI:0915”(physical association)	0.950
BIRC2	CASP9	psi-mi:“MI:0915”(physical association)	0.920
CASP9	BIRC2	psi-mi:“MI:0915”(physical association)	0.920
BIRC2	DIABLO	psi-mi:“MI:0915”(physical association)	0.870
BIRC7	BIRC2	psi-mi:“MI:0915”(physical association)	0.800
BIRC2	NTAQ1	psi-mi:“MI:0915”(physical association)	0.800
BIRC2	BIRC7	psi-mi:“MI:0915”(physical association)	0.800
NTAQ1	BIRC2	psi-mi:“MI:0915”(physical association)	0.800
TRAF1	BIRC2	psi-mi:“MI:0915”(physical association)	0.800
BIRC2	BOLA1	psi-mi:“MI:0915”(physical association)	0.780
BOLA1	BIRC2	psi-mi:“MI:0915”(physical association)	0.780
RIPK1	BIRC2	psi-mi:“MI:0915”(physical association)	0.770
BIRC2	RIPK1	psi-mi:“MI:0915”(physical association)	0.770
TRAF2	HTRA2	psi-mi:“MI:0914”(association)	0.750

BioGRID (613): BIRC2 (Co-crystal Structure), BIRC2 (Affinity Capture-Western), DIABLO (Affinity Capture-Western), MAP3K14 (Affinity Capture-Western), RAC1 (Affinity Capture-Western), RAC1 (Affinity Capture-Luminescence), BIRC2 (Affinity Capture-MS), BIRC2 (Affinity Capture-Western), PCSK9 (Affinity Capture-Western), PCSK9 (Reconstituted Complex), PCSK9 (Biochemical Activity), BIRC2 (Affinity Capture-Western), CASP9 (Two-hybrid), GFAP (Two-hybrid), NMB (Two-hybrid)

ESM2 similar proteins: A1E2V0, A5D8Q0, A9JTP3, A9ULZ2, B1B1A0, O08863, O62640, P33279, P36406, P36407, P42573, P51784, P98170, Q13049, Q13075, Q13489, Q13490, Q1L8G6, Q24307, Q4R8E0, Q5BKL8, Q60989, Q62210, Q63185, Q6P5D3, Q6ZPS6, Q6ZUJ8, Q7Z2W4, Q80Z32, Q8C7M3, Q8CH72, Q8JHV9, Q8K337, Q8N1W1, Q8R151, Q90660, Q95M71, Q95M72, Q96P09, Q9BQI3

Diamond homologs: A1E2V0, A1L020, A1L3F4, A5D8Q0, A9JTP3, A9ULZ2, D3ZDI6, E3SCZ8, O08863, O10296, O10324, O14064, O15392, O62640, O70201, O88738, P40629, P41435, P41436, P41437, P41454, P47732, P98170, Q05AK5, Q0WPJ7, Q13489, Q13490, Q28ER3, Q28H51, Q50L39, Q557E7, Q5BKL8, Q5R881, Q5RAH9, Q60989, Q62210, Q69Z36, Q6I6F4, Q6J1J1, Q6NTT6

SIGNOR signaling

36 interactions.

A	Effect	B	Mechanism
BIRC2	“down-regulates quantity by destabilization”	BIRC2	ubiquitination
DIABLO	“down-regulates quantity”	BIRC2	binding
BIRC2	“up-regulates activity”	RIPK1	ubiquitination
BIRC2	down-regulates	CASP2	binding
XAF1	down-regulates	BIRC2	binding
BIRC2	“down-regulates quantity by destabilization”	TRAF2	ubiquitination
TRAF2	“up-regulates activity”	BIRC2	binding
AT-406	down-regulates	BIRC2	“chemical inhibition”
BIRC3	“up-regulates activity”	BIRC2	binding
BIRC2	“down-regulates quantity by destabilization”	UBE2J1	ubiquitination
Ub:E2	“up-regulates activity”	BIRC2	ubiquitination
BIRC2	“down-regulates quantity by destabilization”	DIABLO	ubiquitination
SCF-FBW7	“down-regulates quantity by destabilization”	BIRC2	ubiquitination
BIRC2	“down-regulates quantity by destabilization”	RIPK1	polyubiquitination
BIRC2	“up-regulates activity”	RIPK4	polyubiquitination
BIRC2	“up-regulates activity”	RIPK1	polyubiquitination
BIRC2	“up-regulates activity”	RIPK3	polyubiquitination
BIRC2	“up-regulates activity”	RIPK2	polyubiquitination
BIRC2	“down-regulates quantity by destabilization”	CSE1L	polyubiquitination
BIRC2	“up-regulates activity”	ENDOG	ubiquitination
BIRC2	“down-regulates quantity”	CFLAR	ubiquitination
BIRC2	“up-regulates activity”	E2F1	ubiquitination
BIRC2	“down-regulates quantity by destabilization”	EIF4E	ubiquitination
BIRC2	“down-regulates quantity by destabilization”	PACS2	ubiquitination

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 106 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
TNFR1-induced proapoptotic signaling	8	48.1×	5e-10
TNF signaling	8	46.4×	5e-10
TNF receptor superfamily (TNFSF) members mediating non-canonical NF-kB pathway	5	46.0×	2e-06
RIPK1-mediated regulated necrosis	7	43.8×	2e-08
Regulation of necroptotic cell death	7	42.1×	2e-08
TNFR1-induced NF-kappa-B signaling pathway	9	41.4×	1e-10
TICAM1, RIP1-mediated IKK complex recruitment	5	41.2×	4e-06
Regulation of TNFR1 signaling	12	36.8×	1e-13

GO biological processes:

GO term	Partners	Fold	FDR
positive regulation of execution phase of apoptosis	5	45.3×	6e-06
canonical NF-kappaB signal transduction	9	35.5×	3e-09
extrinsic apoptotic signaling pathway via death domain receptors	6	25.9×	9e-06
tumor necrosis factor-mediated signaling pathway	7	24.9×	2e-06
positive regulation of extrinsic apoptotic signaling pathway	5	24.5×	1e-04
extrinsic apoptotic signaling pathway	7	23.1×	2e-06
positive regulation of neuron apoptotic process	7	20.5×	5e-06
positive regulation of protein ubiquitination	8	18.4×	2e-06

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	81
Likely benign	5
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

1068 predictions. Top by Δscore:

Variant	Effect	Δscore
11:102347373:TGCGG:T	donor_loss	1.0000
11:102347374:GCG:G	donor_gain	1.0000
11:102347374:GCGGT:G	donor_loss	1.0000
11:102347376:GGTG:G	donor_loss	1.0000
11:102347377:G:C	donor_loss	1.0000
11:102347377:G:GG	donor_gain	1.0000
11:102347378:T:G	donor_loss	1.0000
11:102348685:GGA:G	donor_gain	1.0000
11:102362890:TTTTA:T	acceptor_loss	1.0000
11:102362891:TTTA:T	acceptor_loss	1.0000
11:102362892:TTA:T	acceptor_loss	1.0000
11:102362893:TA:T	acceptor_loss	1.0000
11:102362894:A:AG	acceptor_gain	1.0000
11:102362894:A:AT	acceptor_loss	1.0000
11:102362895:G:GG	acceptor_gain	1.0000
11:102362895:GGT:G	acceptor_gain	1.0000
11:102362895:GGTGT:G	acceptor_gain	1.0000
11:102362971:ACAG:A	donor_loss	1.0000
11:102362973:AGGT:A	donor_loss	1.0000
11:102362975:GT:G	donor_loss	1.0000
11:102362976:T:G	donor_loss	1.0000
11:102363667:GCT:G	acceptor_gain	1.0000
11:102363717:GTAT:G	donor_gain	1.0000
11:102368301:A:G	acceptor_gain	1.0000
11:102368302:ATAGT:A	acceptor_loss	1.0000
11:102368303:TAGT:T	acceptor_loss	1.0000
11:102368304:A:AG	acceptor_gain	1.0000
11:102368304:AGTT:A	acceptor_loss	1.0000
11:102368305:G:GG	acceptor_gain	1.0000
11:102368305:GTT:G	acceptor_gain	1.0000

AlphaMissense

4102 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
11:102350894:T:A	W316R	1.000
11:102350894:T:C	W316R	1.000
11:102350896:G:C	W316C	1.000
11:102350896:G:T	W316C	1.000
11:102378100:T:C	C592R	1.000
11:102378130:T:C	C602R	1.000
11:102350001:A:C	R49S	0.999
11:102350001:A:T	R49S	0.999
11:102350101:T:C	C83R	0.999
11:102350542:T:A	W230R	0.999
11:102350542:T:C	W230R	0.999
11:102350544:G:C	W230C	0.999
11:102350544:G:T	W230C	0.999
11:102350864:T:C	C306R	0.999
11:102350886:T:C	L313S	0.999
11:102350895:G:C	W316S	0.999
11:102350928:C:A	A327D	0.999
11:102350933:T:A	W329R	0.999
11:102350933:T:C	W329R	0.999
11:102350936:T:C	F330L	0.999
11:102350938:T:A	F330L	0.999
11:102350938:T:G	F330L	0.999
11:102362897:T:C	C333R	0.999
11:102378037:T:A	C571S	0.999
11:102378037:T:C	C571R	0.999
11:102378038:G:A	C571Y	0.999
11:102378038:G:C	C571S	0.999
11:102378039:T:G	C571W	0.999
11:102378042:A:C	K572N	0.999
11:102378042:A:T	K572N	0.999

dbSNP variants (sampled 300 via entrez): RS1000128689 (11:102355443 T>A,C), RS1000222744 (11:102378614 T>C), RS1000380121 (11:102373824 T>C), RS1000432247 (11:102374171 CAA>C), RS1000454404 (11:102361430 G>A,C,T), RS1000515957 (11:102356700 A>C,G), RS1000538838 (11:102356901 C>T), RS1000676552 (11:102345321 T>C), RS1000743093 (11:102345531 A>G), RS1000831988 (11:102368243 G>C), RS1000849881 (11:102368748 A>G), RS1000904010 (11:102368934 T>C), RS1000987713 (11:102361862 T>C), RS1001061537 (11:102362655 T>C), RS1001393206 (11:102374872 C>G,T)

Disease associations

OMIM: gene MIM:601712 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST001942_2	Prostate cancer	2.000000e-11

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (32): CHEMBL2221342 (PROTEIN COMPLEX), CHEMBL3038465 (PROTEIN FAMILY), CHEMBL3885521 (PROTEIN COMPLEX), CHEMBL4296118 (PROTEIN-PROTEIN INTERACTION), CHEMBL4296119 (PROTEIN-PROTEIN INTERACTION), CHEMBL4630748 (PROTEIN-PROTEIN INTERACTION), CHEMBL4630749 (PROTEIN-PROTEIN INTERACTION), CHEMBL4680047 (PROTEIN-PROTEIN INTERACTION), CHEMBL4802030 (PROTEIN-PROTEIN INTERACTION), CHEMBL4802031 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

5 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 3,611 (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
CHEMBL2158051	XEVINAPANT	3	680
CHEMBL2431768	LCL-161	2	1,365
CHEMBL3039522	BIRINAPANT	2	925
CHEMBL2063869	GDC-0152	1	281
CHEMBL4173974	ASTX-660	1	360

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: other protein — Inhibitors of apoptosis (IAP) protein family

Most potent curated ligand interactions (10 total), top 10:

Ligand	Action	Affinity	Parameter
tolinapant	Inhibition	9.66	pIC50
birinapant	Antagonist	9.0	pKd
SM-122	Inhibition	9.0	pKi
SM-337	Antagonist	8.82	pKi
xevinapant	Antagonist	8.72	pKi
AZD5582	Antagonist	7.82	pIC50
GDC-0152	Antagonist	7.77	pKi
BV-6	Inhibition	7.54	pKd
LCL161	Inhibition	7.24	pIC50
compound 20 [PMID: 34432979]	Binding	7.1	pIC50

Binding affinities (BindingDB)

840 measured of 920 human assays (920 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
methyl (8R,12S,15S,18S,29R,33S,36S,39S)-39-cyano-11,32-bis[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-15,36-bis(naphthalen-2-ylmethyl)-13,16,34,37-tetraoxo-2,23-dioxa-5,6,7,11,14,17,26,27,28,32,35,38-dodecazaheptacyclo[39.2.2.219,22.14,7.125,28.08,12.029,33]nonatetraconta-1(44),4(49),5,19,21,25(46),26,41(45),42,47-decaene-18-carboxylate	IC50	0.3 nM	US-9605022: Macrocyclic compounds for inhibition of inhibitors of apoptosis
(8R,12S,15S,18R,30R,34S,37S,40S)-11,33-bis[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-15,37-bis(naphthalen-2-ylmethyl)-13,16,35,38-tetraoxo-40-(5-oxo-1,2,4-oxadiazolidin-3-yl)-2,24-dioxa-5,6,7,11,14,17,27,28,29,33,36,39-dodecazaheptacyclo[40.2.2.220,23.14,7.126,29.08,12.030,34]pentaconta-1(45),4(50),5,20,22,26(47),27,42(46),43,48-decaene-18-carboxylic acid	IC50	0.4 nM	US-9605022: Macrocyclic compounds for inhibition of inhibitors of apoptosis
(4R,8S,11S,14R,24R,28S,31S,34R)-7,27-bis[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-11,31-bis(naphthalen-2-ylmethyl)-9,12,29,32-tetraoxo-3,23-dioxa-7,10,13,18,19,20,27,30,33,38,39,40-dodecazapentacyclo[36.2.1.118,21.04,8.024,28]dotetraconta-1(41),19,21(42),39-tetraene-14,34-dicarboxylic acid	IC50	0.8 nM	US-9605022: Macrocyclic compounds for inhibition of inhibitors of apoptosis
(8R,12S,15S,18R,30R,34S,37S,40S)-11,33-bis[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-15,37-bis(naphthalen-2-ylmethyl)-13,16,35,38-tetraoxo-40-(5-sulfanylidene-1,2,4-oxadiazolidin-3-yl)-2,24-dioxa-5,6,7,11,14,17,27,28,29,33,36,39-dodecazaheptacyclo[40.2.2.220,23.14,7.126,29.08,12.030,34]pentaconta-1(45),4(50),5,20,22,26(47),27,42(46),43,48-decaene-18-carboxylic acid	IC50	0.8 nM	US-9605022: Macrocyclic compounds for inhibition of inhibitors of apoptosis
(2R)-N-[4-(1,3-dimethylpyrazolo[4,5-d]pyrimidin-7-yl)-6-[2-(1-methylindazol-5-yl)ethynyl]-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-N-[4-(1,3-dimethylpyrazolo[4,5-d]pyrimidin-7-yl)-6-[2-(1-methylisoquinolin-6-yl)ethynyl]-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-N-[4-(1,3-dimethylpyrazolo[4,5-d]pyrimidin-7-yl)-6-[2-(8-fluoro-2-methylquinolin-4-yl)ethynyl]-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-N-[4-(1,3-dimethylpyrazolo[4,5-d]pyrimidin-7-yl)-6-[2-(3-methylimidazo[1,5-a]pyridin-7-yl)ethynyl]-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-2-(methylamino)-N-[6-[2-(1-methylisoquinolin-6-yl)ethynyl]-4-(1-methylpyrazolo[4,5-d]pyrimidin-7-yl)-2-pyridinyl]propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-2-(methylamino)-N-[6-[2-(1-methyl-2-oxoquinolin-6-yl)ethynyl]-4-(1-methylpyrazolo[4,5-d]pyrimidin-7-yl)-2-pyridinyl]propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-N-[4-(2,3-dimethylimidazo[1,2-a]pyridin-5-yl)-6-[2-(1-methylisoquinolin-6-yl)ethynyl]-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-2-(methylamino)-N-[4-(5-methylimidazo[1,2-a]pyridin-3-yl)-6-[2-(1-methylisoquinolin-6-yl)ethynyl]-2-pyridinyl]propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-2-(methylamino)-N-[6-[2-(1-methylisoquinolin-6-yl)ethynyl]-4-(1,2,4,6-tetramethyl-3-oxopyrazolo[4,3-c]pyridin-7-yl)-2-pyridinyl]propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-2-(methylamino)-N-[6-[2-(1-methyl-2-oxoquinolin-6-yl)ethynyl]-4-(1,3,5-trimethylpyrazolo[4,5-d]pyrimidin-7-yl)-2-pyridinyl]propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-2-(methylamino)-N-[6-[2-(1-methylisoquinolin-6-yl)ethynyl]-4-(1,3,5-trimethylpyrazolo[4,5-d]pyrimidin-7-yl)-2-pyridinyl]propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-2-(methylamino)-N-[6-[2-(1-methylindazol-5-yl)ethynyl]-4-(1,3,5-trimethylpyrazolo[4,5-d]pyrimidin-7-yl)-2-pyridinyl]propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-2-(methylamino)-N-[6-[2-(1-methylisoquinolin-6-yl)ethynyl]-4-(2,3,6-trimethylpyrazolo[3,4-d]pyrimidin-4-yl)-2-pyridinyl]propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-2-(methylamino)-N-[6-[2-(1-methylindazol-5-yl)ethynyl]-4-(2,3,6-trimethylpyrazolo[3,4-d]pyrimidin-4-yl)-2-pyridinyl]propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-2-(methylamino)-N-[6-[2-[2-(4-methylimidazol-1-yl)pyrimidin-5-yl]ethynyl]-4-(2,3,6-trimethylpyrazolo[3,4-d]pyrimidin-4-yl)-2-pyridinyl]propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-2-(methylamino)-N-[6-(2-thiophen-2-ylethynyl)-4-(2,3,6-trimethylpyrazolo[3,4-d]pyrimidin-4-yl)-2-pyridinyl]propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
N-[4-(1,3-dimethylpyrazolo[4,5-d]pyrimidin-7-yl)-6-[2-(2-methylquinolin-6-yl)ethynyl]-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
N-[4-(1,3-dimethylpyrazolo[4,5-d]pyrimidin-7-yl)-6-[2-(2,6-dimethyl-4-pyridinyl)ethynyl]-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
N-[6-[2-(3,5-difluorophenyl)ethynyl]-4-(1,3-dimethylpyrazolo[4,5-d]pyrimidin-7-yl)-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
N-[4-(1,3-dimethylpyrazolo[4,5-d]pyrimidin-7-yl)-6-[2-[4-(4-methylimidazol-1-yl)phenyl]ethynyl]-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
N-[4-(1,3-dimethylpyrazolo[4,5-d]pyrimidin-7-yl)-6-[2-(8-fluoroquinolin-6-yl)ethynyl]-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
N-[4-(1,3-dimethylpyrazolo[4,5-d]pyrimidin-7-yl)-6-[2-(1-methylpyrazolo[5,4-b]pyridin-5-yl)ethynyl]-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9278978: 6-Alkynyl Pyridine
(2S)-N-[5-[2-(2-methoxy-3-pyridinyl)-7-methylimidazo[1,2-a]pyridin-3-yl]-6-[2-(1-methylisoquinolin-6-yl)ethynyl]-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9481673: 6-alkynyl-pyridine derivatives
(2S)-2-(methylamino)-N-[6-[2-(1-methylisoquinolin-6-yl)ethynyl]-5-[7-methyl-2-(2-methyl-4-pyridinyl)imidazo[1,2-a]pyridin-3-yl]-2-pyridinyl]propanamide	IC50	1 nM	US-9481673: 6-alkynyl-pyridine derivatives
(2S)-2-(methylamino)-N-[6-[2-(1-methylisoquinolin-6-yl)ethynyl]-5-[7-methyl-2-(1-methylpyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]-2-pyridinyl]propanamide	IC50	1 nM	US-9481673: 6-alkynyl-pyridine derivatives
(2S)-2-(methylamino)-N-[6-[2-(1-methylisoquinolin-6-yl)ethynyl]-5-[7-methyl-2-(3-methylimidazol-4-yl)imidazo[1,2-a]pyridin-3-yl]-2-pyridinyl]propanamide	IC50	1 nM	US-9481673: 6-alkynyl-pyridine derivatives
(2S)-2-(methylamino)-N-[6-[2-(1-methylisoquinolin-6-yl)ethynyl]-5-[7-methyl-2-(6-methyl-3-pyridinyl)imidazo[1,2-a]pyridin-3-yl]-2-pyridinyl]propanamide	IC50	1 nM	US-9481673: 6-alkynyl-pyridine derivatives
(2S)-2-(methylamino)-N-[6-[2-(1-methylisoquinolin-6-yl)ethynyl]-5-[7-methyl-2-(2-methylpyrimidin-5-yl)imidazo[1,2-a]pyridin-3-yl]-2-pyridinyl]propanamide	IC50	1 nM	US-9481673: 6-alkynyl-pyridine derivatives
(2S)-N-[5-[2-(2-methoxy-4-pyridinyl)-7-methylimidazo[1,2-a]pyridin-3-yl]-6-[2-(1-methylisoquinolin-6-yl)ethynyl]-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9481673: 6-alkynyl-pyridine derivatives
(2S)-N-[5-[2-(6-methoxy-3-pyridinyl)-7-methylimidazo[1,2-a]pyridin-3-yl]-6-[2-(1-methylisoquinolin-6-yl)ethynyl]-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9481673: 6-alkynyl-pyridine derivatives
(2S)-N-[5-[2-(2-methoxy-3-pyridinyl)-7-methylimidazo[1,2-a]pyridin-3-yl]-6-[2-(1-methyl-2-oxoquinolin-6-yl)ethynyl]-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9481673: 6-alkynyl-pyridine derivatives
(2S)-2-(methylamino)-N-[5-[7-methyl-2-(2-methyl-4-pyridinyl)imidazo[1,2-a]pyridin-3-yl]-6-(2-phenylethynyl)-2-pyridinyl]propanamide	IC50	1 nM	US-9481673: 6-alkynyl-pyridine derivatives
(2S)-N-[5-[2-(2-methoxy-4-pyridinyl)-7-methylimidazo[1,2-a]pyridin-3-yl]-6-[2-(1-methyl-2-oxoquinolin-6-yl)ethynyl]-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9481673: 6-alkynyl-pyridine derivatives
(2S)-N-[5-[2-(6-methoxy-3-pyridinyl)-7-methylimidazo[1,2-a]pyridin-3-yl]-6-[2-(1-methyl-2-oxoquinolin-6-yl)ethynyl]-2-pyridinyl]-2-(methylamino)propanamide	IC50	1 nM	US-9481673: 6-alkynyl-pyridine derivatives
(2R,5S,8S)-8-[(2S)-2-(methylamino)propanamido]-7-oxo-N-[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]-6-azatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),11,13-triene-5-carboxamide	KI	1.1 nM
(8R,12S,15S,18S,30R,34S,37S,40S)-11,33-bis[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-15,37-bis(naphthalen-2-ylmethyl)-13,16,35,38-tetraoxo-2,24-dioxa-5,6,7,11,14,17,27,28,29,33,36,39-dodecazaheptacyclo[40.2.2.220,23.14,7.126,29.08,12.030,34]pentaconta-1(45),4(50),5,20,22,26(47),27,42(46),43,48-decaene-18,40-dicarboxylic acid	IC50	1.1 nM	US-9605022: Macrocyclic compounds for inhibition of inhibitors of apoptosis
(8R,12S,15S,18S,30R,34S,39R,42S)-42-[(3,5-difluoro-4-hydroxyphenyl)methylcarbamoyl]-11,33-bis[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-15,39-bis(naphthalen-2-ylmethyl)-13,16,35,37,40-pentaoxo-2,24-dioxa-5,6,7,11,14,17,27,28,29,33,36,41-dodecazaheptacyclo[42.2.2.220,23.14,7.126,29.08,12.030,34]dopentaconta-1(47),4(52),5,20,22,26(49),27,44(48),45,50-decaene-18-carboxylic acid	IC50	1.2 nM	US-9605022: Macrocyclic compounds for inhibition of inhibitors of apoptosis
BMC175834 Compound 1b	KI	1.3 nM
(8R,12S,15S,18S,30R,34S,37S,40S)-40-(cyclopropylsulfonylcarbamoyl)-11,33-bis[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-15,37-bis(naphthalen-2-ylmethyl)-13,16,35,38-tetraoxo-2,24-dioxa-5,6,7,11,14,17,27,28,29,33,36,39-dodecazaheptacyclo[40.2.2.220,23.14,7.126,29.08,12.030,34]pentaconta-1(45),4(50),5,20,22,26(47),27,42(46),43,48-decaene-18-carboxylic acid	IC50	1.3 nM	US-9605022: Macrocyclic compounds for inhibition of inhibitors of apoptosis
(8R,12S,15S,18S,30R,34S,39R,42S)-11,33-bis[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-15,39-bis(naphthalen-2-ylmethyl)-13,16,35,37,40-pentaoxo-18-(2-oxo-3H-1,3,4-oxadiazol-5-yl)-2,24-dioxa-5,6,7,11,14,17,27,28,29,33,36,41-dodecazaheptacyclo[42.2.2.220,23.14,7.126,29.08,12.030,34]dopentaconta-1(47),4(52),5,20,22,26(49),27,44(48),45,50-decaene-42-carboxylic acid	IC50	1.3 nM	US-9605022: Macrocyclic compounds for inhibition of inhibitors of apoptosis
(8R,12S,15S,18S,30R,34S,39R,42S)-42-[[(3R,5R)-6-carboxy-3,5-dihydroxyhexyl]carbamoyl]-11,33-bis[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-15,39-bis(naphthalen-2-ylmethyl)-13,16,35,37,40-pentaoxo-2,24-dioxa-5,6,7,11,14,17,27,28,29,33,36,41-dodecazaheptacyclo[42.2.2.220,23.14,7.126,29.08,12.030,34]dopentaconta-1(47),4(52),5,20,22,26(49),27,44(48),45,50-decaene-18-carboxylic acid	IC50	1.4 nM	US-9605022: Macrocyclic compounds for inhibition of inhibitors of apoptosis
(4R,8S,11S,16S,23R,27S,30S,35S)-7,26-bis[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-11,30-bis(naphthalen-2-ylmethyl)-9,12,28,31-tetraoxo-3,22-dioxa-7,10,13,17,18,19,26,29,32,36,37,38-dodecazapentacyclo[34.2.1.117,20.04,8.023,27]tetraconta-1(39),18,20(40),37-tetraene-16,35-dicarboxylic acid	IC50	1.6 nM	US-9605022: Macrocyclic compounds for inhibition of inhibitors of apoptosis
(2R)-2-(methylamino)-N-[4-(1-methylpyrazolo[4,5-d]pyrimidin-7-yl)-6-(2-phenylethynyl)-2-pyridinyl]propanamide	IC50	2 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-2-(methylamino)-N-[6-[2-[4-(4-methylimidazol-1-yl)phenyl]ethynyl]-4-(1-methylpyrazolo[4,5-d]pyrimidin-7-yl)-2-pyridinyl]propanamide	IC50	2 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-N-[4-(5,6-dimethylfuro[2,3-d]pyrimidin-4-yl)-6-(2-phenylethynyl)-2-pyridinyl]-2-(methylamino)propanamide	IC50	2 nM	US-9278978: 6-Alkynyl Pyridine
(2R)-2-(methylamino)-N-[6-[2-(1-methyl-2-oxoquinolin-6-yl)ethynyl]-4-(2,3,6-trimethylpyrazolo[3,4-d]pyrimidin-4-yl)-2-pyridinyl]propanamide	IC50	2 nM	US-9278978: 6-Alkynyl Pyridine

ChEMBL bioactivities

934 potent at pChembl≥5 of 972 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.00	EC50	0.1	nM	CHEMBL3108819
10.00	EC50	0.1	nM	CHEMBL3108817
10.00	EC50	0.1	nM	CHEMBL3108827
10.00	IC50	0.1	nM	CHEMBL4166057
10.00	EC50	0.1	nM	CHEMBL3108931
9.89	IC50	0.13	nM	CHEMBL4167141
9.77	IC50	0.17	nM	CHEMBL4171490
9.74	IC50	0.18	nM	CHEMBL4169478
9.72	IC50	0.19	nM	CHEMBL4166607
9.70	EC50	0.2	nM	CHEMBL3108821
9.70	EC50	0.2	nM	CHEMBL3108818
9.70	EC50	0.2	nM	CHEMBL3108920
9.70	EC50	0.2	nM	CHEMBL3108927
9.70	IC50	0.2	nM	CHEMBL4164271
9.66	IC50	0.22	nM	ASTX-660
9.52	EC50	0.3	nM	CHEMBL3108922
9.52	IC50	0.3	nM	CHEMBL5916145
9.49	IC50	0.32	nM	CHEMBL234346
9.49	EC50	0.32	nM	CHEMBL4064619
9.49	IC50	0.32	nM	CHEMBL4064619
9.47	IC50	0.34	nM	CHEMBL4160872
9.43	Ki	0.37	nM	CHEMBL475670
9.40	Ki	0.4	nM	CHEMBL2158601
9.40	EC50	0.4	nM	CHEMBL3108931
9.40	EC50	0.4	nM	LCL-161
9.40	IC50	0.4	nM	LCL-161
9.40	IC50	0.4	nM	CHEMBL5806178
9.30	Ki	0.5	nM	CHEMBL1774154
9.30	EC50	0.5	nM	CHEMBL3108919
9.23	IC50	0.59	nM	CHEMBL4159232
9.22	EC50	0.6	nM	CHEMBL3108820
9.22	EC50	0.6	nM	CHEMBL3108921
9.22	EC50	0.6	nM	CHEMBL3108929
9.21	IC50	0.62	nM	CHEMBL4168197
9.17	Ki	0.68	nM	CHEMBL481213
9.15	Kd	0.7	nM	CHEMBL2158054
9.15	Ki	0.7	nM	CHEMBL2158600
9.15	IC50	0.7	nM	CHEMBL4177336
9.13	IC50	0.74	nM	CHEMBL4174922
9.10	Ki	0.8	nM	CHEMBL481422
9.10	IC50	0.8	nM	CHEMBL5799178
9.10	IC50	0.8	nM	CHEMBL5984721
9.00	IC50	1	nM	CHEMBL3094405
9.00	IC50	1	nM	CHEMBL3935993
9.00	IC50	1	nM	CHEMBL3975889
9.00	IC50	1	nM	CHEMBL3932853
9.00	IC50	1	nM	CHEMBL3946504
9.00	IC50	1	nM	CHEMBL3916269
9.00	IC50	1	nM	CHEMBL3915777
9.00	IC50	1	nM	CHEMBL3928237

PubChem BioAssay actives

488 with measured affinity, of 824 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
1-[2-[(2R,5R)-2-[[(3R,5R)-3,5-dimethylmorpholin-4-yl]methyl]-5-methylpiperazin-1-yl]acetyl]-6-[(4-fluorophenyl)methyl]-3,3-dimethyl-2,4-dihydropyrrolo[3,2-b]pyridin-5-one	1362434: Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs	ic50	0.0001	uM
2-[(2R,5R)-2-[[(3R,5R)-3,5-dimethylmorpholin-4-yl]methyl]-5-methylpiperazin-1-yl]-1-[6-[(4-fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-1-yl]ethanone	1362434: Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs	ic50	0.0001	uM
(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-[(1S,2R)-2-[6-[[(1S,2R)-1-[[(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-2,3-dihydro-1H-inden-2-yl]oxy]hexoxy]-2,3-dihydro-1H-inden-1-yl]pyrrolidine-2-carboxamide	1066126: Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA	ec50	0.0001	uM
(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-[(1S,2R)-2-[6-[[(1S,2R)-1-[[(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-2,3-dihydro-1H-inden-2-yl]oxy]hexa-2,4-diynoxy]-2,3-dihydro-1H-inden-1-yl]pyrrolidine-2-carboxamide	1066126: Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA	ec50	0.0001	uM
(1S,3S,5S)-2-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-[(1S,2R)-2-[6-[[(1S,2R)-1-[[(1S,3S,5S)-2-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonyl]amino]-2,3-dihydro-1H-inden-2-yl]oxy]hexa-2,4-diynoxy]-2,3-dihydro-1H-inden-1-yl]-2-azabicyclo[3.1.0]hexane-3-carboxamide	1066126: Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA	ec50	0.0001	uM
(2S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-N-[(1S,2R)-2-[6-[[(1S,2R)-1-[[(2S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-2,3-dihydro-1H-inden-2-yl]oxy]hexa-2,4-diynoxy]-2,3-dihydro-1H-inden-1-yl]pyrrolidine-2-carboxamide	1553577: Induction of cIAP1 (unknown origin) degradation	ec50	0.0001	uM
1-[6-[(4-fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-1-yl]-2-[(2R,5R)-5-methyl-2-[[(3R)-3-methylmorpholin-4-yl]methyl]piperazin-1-yl]ethanone	1362434: Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs	ic50	0.0002	uM
1-[2-[(2R,5R)-2-[[(3R,5R)-3,5-dimethylmorpholin-4-yl]methyl]-5-methylpiperazin-1-yl]acetyl]-6-[(4-fluorophenyl)methyl]-3,3,4-trimethyl-2H-pyrrolo[3,2-b]pyridin-5-one	1362434: Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs	ic50	0.0002	uM
(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-[(1S,2S)-2-[6-[[(1S,2S)-1-[[(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-2,3-dihydro-1H-inden-2-yl]oxy]hexa-2,4-diynoxy]-2,3-dihydro-1H-inden-1-yl]pyrrolidine-2-carboxamide	1066126: Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA	ec50	0.0002	uM
2-[(2R,5R)-2-[[(3R,5R)-3,5-dimethylmorpholin-4-yl]methyl]-5-methylpiperazin-1-yl]-1-[6-[(4-fluorophenyl)methyl]-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-1-yl]ethanone	1362434: Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs	ic50	0.0002	uM
2-[[(2R,5R)-1-[2-[3-[(2,4-difluorophenyl)methyl]-7,7-dimethyl-6H-pyrrolo[3,2-c]pyridazin-5-yl]-2-oxoethyl]-5-methylpiperazin-2-yl]methyl]-4-fluoro-3H-isoindol-1-one	1362434: Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs	ic50	0.0002	uM
2-[[(2R,5R)-1-[2-[3-[(2,4-difluorophenyl)methyl]-7,7-dimethyl-6H-pyrrolo[3,2-c]pyridazin-5-yl]-2-oxoethyl]-5-methylpiperazin-2-yl]methyl]-5-fluoro-3H-isoindol-1-one	1362434: Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs	ic50	0.0002	uM
(4R)-3-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-[(1S,2R)-2-[6-[[(1S,2R)-1-[[(4R)-3-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-1,3-thiazolidine-4-carbonyl]amino]-2,3-dihydro-1H-inden-2-yl]oxy]hexa-2,4-diynoxy]-2,3-dihydro-1H-inden-1-yl]-1,3-thiazolidine-4-carboxamide	1066126: Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA	ec50	0.0002	uM
(2S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-N-[(1S,2R)-2-[6-[[(1S,2R)-1-[[(2S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-1,2,3,4-tetrahydronaphthalen-2-yl]oxy]hexa-2,4-diynoxy]-1,2,3,4-tetrahydronaphthalen-1-yl]pyrrolidine-2-carboxamide	1066126: Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA	ec50	0.0002	uM
(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-[(4R)-1-[6-[(4R)-4-[[(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-3,4-dihydro-2H-quinolin-1-yl]hexa-2,4-diynyl]-3,4-dihydro-2H-quinolin-4-yl]pyrrolidine-2-carboxamide	1066126: Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA	ec50	0.0002	uM
(2S,3S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoic acid	1448026: Inhibition of SMAC-derived peptide abuRPFK (5 and 6FAM)-amide interaction with cIAP1 BIR3 domain (unknown origin) by fluorescence polarization assay	ic50	0.0003	uM
1-[6-[(4-fluorophenyl)methyl]-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-1-yl]-2-[(2R,5R)-5-methyl-2-[[(3R)-3-methylmorpholin-4-yl]methyl]piperazin-1-yl]ethanone	1362434: Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs	ic50	0.0003	uM
2-[[(2R,5R)-1-[2-[3-[(2,4-difluorophenyl)methyl]-7,7-dimethyl-6H-pyrrolo[3,2-c]pyridazin-5-yl]-2-oxoethyl]-5-methylpiperazin-2-yl]methyl]-3H-isoindol-1-one	1362434: Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs	ic50	0.0003	uM
(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-[(1S,2R)-2-[6-[[(1S,2R)-1-[[(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-2,5-dihydropyrrole-2-carbonyl]amino]-2,3-dihydro-1H-inden-2-yl]oxy]hexa-2,4-diynoxy]-2,3-dihydro-1H-inden-1-yl]-2,5-dihydropyrrole-2-carboxamide	1066126: Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA	ec50	0.0003	uM
(2S)-N-[(1S)-1-cyclohexyl-2-[(2S)-2-[4-(4-fluorobenzoyl)-1,3-thiazol-2-yl]pyrrolidin-1-yl]-2-oxoethyl]-2-(methylamino)propanamide	1362434: Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs	ic50	0.0004	uM
(1S,3S,6S,10aS)-1-benzyl-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-N-[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide	368236: Displacement of fluorescent SM5F peptide from His-tagged human cIAP1 BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay	ki	0.0004	uM
(5S,8S,10aR)-3-[6-[(5S,8S,10aR)-8-(benzhydrylcarbamoyl)-5-[[(2S)-2-(methylamino)propanoyl]amino]-6-oxo-1,2,4,5,8,9,10,10a-octahydropyrrolo[1,2-a][1,5]diazocin-3-yl]-6-oxohexanoyl]-N-benzhydryl-5-[[(2S)-2-(methylamino)propanoyl]amino]-6-oxo-1,2,4,5,8,9,10,10a-octahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide	694873: Binding affinity to BIR3 domain of cIAP1 by fluorescence polarization assay	ki	0.0004	uM
(3S,6S,10aS)-N-[(S)-[1-[4-[4-[4-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]butyl]phenyl]butyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide	694873: Binding affinity to BIR3 domain of cIAP1 by fluorescence polarization assay	ki	0.0005	uM
(3S,6S,10aS)-N-[(S)-[1-[8-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]octyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide	694873: Binding affinity to BIR3 domain of cIAP1 by fluorescence polarization assay	ki	0.0005	uM
(4R)-3-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-N-[(1S,2R)-2-[6-[[(1S,2R)-1-[[(4R)-3-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-1,3-thiazolidine-4-carbonyl]amino]-2,3-dihydro-1H-inden-2-yl]oxy]hexa-2,4-diynoxy]-2,3-dihydro-1H-inden-1-yl]-1,3-thiazolidine-4-carboxamide	1066126: Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA	ec50	0.0005	uM
2-[(2R,5R)-2-[[(3R,5S)-3,5-dimethylmorpholin-4-yl]methyl]-5-methylpiperazin-1-yl]-1-[6-[(4-fluorophenyl)methyl]-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-1-yl]ethanone	1362434: Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs	ic50	0.0006	uM
2-[(2R,5R)-2-[[(3R,5R)-3,5-dimethylmorpholin-4-yl]methyl]-5-methylpiperazin-1-yl]-1-[6-[(4-fluoro-2-hydroxyphenyl)methyl]-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-1-yl]ethanone	1362434: Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs	ic50	0.0006	uM
(2S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-N-[(1S,2S)-2-[6-[[(1S,2S)-1-[[(2S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-1,2,3,4-tetrahydronaphthalen-2-yl]oxy]hexa-2,4-diynoxy]-1,2,3,4-tetrahydronaphthalen-1-yl]pyrrolidine-2-carboxamide	1066126: Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA	ec50	0.0006	uM
(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-[(1S,2R)-2-[2-[2-[[(1S,2R)-1-[[(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-2,3-dihydro-1H-inden-2-yl]oxy]ethoxy]ethoxy]-2,3-dihydro-1H-inden-1-yl]pyrrolidine-2-carboxamide	1066126: Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA	ec50	0.0006	uM
(7R)-6-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-[(1S,2R)-2-[6-[[(1S,2R)-1-[[(7R)-6-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-4-thia-6-azaspiro[2.4]heptane-7-carbonyl]amino]-2,3-dihydro-1H-inden-2-yl]oxy]hexa-2,4-diynoxy]-2,3-dihydro-1H-inden-1-yl]-4-thia-6-azaspiro[2.4]heptane-7-carboxamide	1066126: Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA	ec50	0.0006	uM
1-[2-[(2R,5R)-2-[[(3R,5R)-3,5-dimethylmorpholin-4-yl]methyl]-5-methylpiperazin-1-yl]acetyl]-6-[(4-fluorophenyl)methyl]-3,3-dimethyl-2H-pyrrolo[2,3-c]pyridin-5-one	1362434: Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs	ic50	0.0007	uM
(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-N-[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide	368236: Displacement of fluorescent SM5F peptide from His-tagged human cIAP1 BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay	ki	0.0007	uM
5-[10-[4-[(S)-[[(5S,8S,10aR)-5-[[(2S)-2-(methylamino)propanoyl]amino]-3-(3-methylbutanoyl)-6-oxo-1,2,4,5,8,9,10,10a-octahydropyrrolo[1,2-a][1,5]diazocine-8-carbonyl]amino]-phenylmethyl]triazol-1-yl]decylcarbamoyl]-2-(3-hydroxy-6-oxoxanthen-9-yl)benzoic acid	695453: Binding affinity to human cIAP1 BIR3 domain expressed in Escherichia coli BL21(DE3) assessed as dissociation constant after 2 to 3 hrs by fluorescence polarization assay	kd	0.0007	uM
(5S,8S,10aR)-3-[4-[(5S,8S,10aR)-8-(benzhydrylcarbamoyl)-5-[[(2S)-2-(methylamino)propanoyl]amino]-6-oxo-1,2,4,5,8,9,10,10a-octahydropyrrolo[1,2-a][1,5]diazocin-3-yl]-4-oxobutanoyl]-N-benzhydryl-5-[[(2S)-2-(methylamino)propanoyl]amino]-6-oxo-1,2,4,5,8,9,10,10a-octahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide	694873: Binding affinity to BIR3 domain of cIAP1 by fluorescence polarization assay	ki	0.0007	uM
2-[[(2R,5R)-1-[2-[3-[(2,4-difluorophenyl)methyl]-7,7-dimethyl-6H-pyrrolo[3,2-c]pyridazin-5-yl]-2-oxoethyl]-5-methylpiperazin-2-yl]methyl]-6-fluoro-3H-isoindol-1-one	1362434: Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs	ic50	0.0007	uM
(3S,6S,10aS)-N-benzhydryl-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide	368236: Displacement of fluorescent SM5F peptide from His-tagged human cIAP1 BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay	ki	0.0008	uM
(3S,6S,9R,10aR)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-9-[(2-phenylacetyl)amino]-N-[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide	511531: Displacement of fluorescent SM5F peptide from His-tagged human cIAP1 BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay	ki	0.0010	uM
(2S)-N-[(2S)-1-[(2R,4S)-2-[[6-fluoro-2-[6-fluoro-3-[[(2R,4S)-4-hydroxy-1-[(2S)-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]pyrrolidin-2-yl]methyl]-1H-indol-2-yl]-1H-indol-3-yl]methyl]-4-hydroxypyrrolidin-1-yl]-1-oxobutan-2-yl]-2-(methylamino)propanamide	1553574: Binding affinity to cIAP1-BIR3 domain (unknown origin)	kd	0.0010	uM
(5S,8S,10aR)-N-[(S)-[1-[10-[6-[5-[(3aS,4S,6aR)-2-oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-4-yl]pentanoylamino]hexanoylamino]decyl]triazol-4-yl]-phenylmethyl]-5-[[(2S)-2-(methylamino)propanoyl]amino]-3-(3-methylbutanoyl)-6-oxo-1,2,4,5,8,9,10,10a-octahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide	695456: Competitive inhibition of human cIAP1 BIR3 domain expressed in Escherichia coli BL21(DE3) after 2 to 3 hrs by fluorescence polarization assay	ki	0.0010	uM
(3S,6S,10aS)-N-[(S)-[1-[2-[4-[2-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]ethyl]phenyl]ethyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide	596635: Binding affinity to human cIAP1 BIR3 domain after 2 to 3 hrs by fluorescence polarization-based assay	ki	0.0010	uM
(3S,6S,10aS)-N-[(S)-[1-[3-[4-[3-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]propyl]phenyl]propyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide	596635: Binding affinity to human cIAP1 BIR3 domain after 2 to 3 hrs by fluorescence polarization-based assay	ki	0.0010	uM
(3S,6S,10aS)-N-[(S)-[1-[6-[4-[6-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]hexyl]phenyl]hexyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide	596635: Binding affinity to human cIAP1 BIR3 domain after 2 to 3 hrs by fluorescence polarization-based assay	ki	0.0010	uM
(3S,6S,10aS)-N-[(S)-[1-[10-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]decyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide	596635: Binding affinity to human cIAP1 BIR3 domain after 2 to 3 hrs by fluorescence polarization-based assay	ki	0.0010	uM
(3S,6S,10aS)-N-[(S)-[1-[12-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]dodecyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide	596635: Binding affinity to human cIAP1 BIR3 domain after 2 to 3 hrs by fluorescence polarization-based assay	ki	0.0010	uM
(3S,6S,10aS)-N-[(S)-[1-[4-[1-[4-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]butyl]triazol-4-yl]butyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide	596635: Binding affinity to human cIAP1 BIR3 domain after 2 to 3 hrs by fluorescence polarization-based assay	ki	0.0010	uM
(3S,6S,10aS)-N-[(S)-[1-[4-[4-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]butylcarbamoylamino]butyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide	596635: Binding affinity to human cIAP1 BIR3 domain after 2 to 3 hrs by fluorescence polarization-based assay	ki	0.0010	uM
(3S,6S,10aS)-N-[(S)-[1-[5-[5-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]pentoxy]pentyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide	596635: Binding affinity to human cIAP1 BIR3 domain after 2 to 3 hrs by fluorescence polarization-based assay	ki	0.0010	uM
(3S,6S,10aS)-N-[(S)-[1-[2-[4-[2-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]ethoxy]butoxy]ethyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide	596635: Binding affinity to human cIAP1 BIR3 domain after 2 to 3 hrs by fluorescence polarization-based assay	ki	0.0010	uM
(3S,10aS)-8-cyano-2-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)butanoyl]amino]acetyl]-N-[(4R)-3,4-dihydro-2H-chromen-4-yl]-3,4,10,10a-tetrahydro-1H-pyrazino[1,2-a]indole-3-carboxamide	1057557: Inhibition of human recombinant His-tagged cIAP-1 BIR3 domain (250 to 350) using AVPIAQ-K(biotin)-NH2 as substrate after overnight incubation by HTRF assay	ic50	0.0010	uM
2-[[(2R,5R)-1-[2-[3-[(2,4-difluorophenyl)methyl]-7,7-dimethyl-6H-pyrrolo[3,2-c]pyridazin-5-yl]-2-oxoethyl]-5-methylpiperazin-2-yl]methyl]-1-oxo-3H-isoindole-5-carbonitrile	1362434: Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs	ic50	0.0010	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Curcumin	decreases expression, decreases reaction, increases expression	8
Resveratrol	increases expression, decreases expression, decreases reaction, affects cotreatment	6
Doxorubicin	affects response to substance, decreases expression, increases expression, decreases reaction	6
Plant Extracts	affects cotreatment, increases expression, decreases reaction, decreases expression, affects expression	5
Tretinoin	decreases expression, increases expression, increases reaction, affects cotreatment	5
Paclitaxel	affects cotreatment, affects response to substance, decreases reaction, increases expression, decreases expression	5
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one	decreases reaction, increases expression, decreases expression	4
Bortezomib	decreases expression, affects cotreatment	4
Etoposide	affects response to substance, decreases response to substance, increases expression	4
sodium arsenite	decreases expression, increases expression	3
Arsenic Trioxide	affects cotreatment, decreases expression, increases reaction	3
Glyphosate	affects cotreatment, decreases expression, decreases response to substance, increases expression	3
Cisplatin	decreases response to substance	3
Simvastatin	decreases expression, decreases reaction, increases expression	3
bisphenol A	affects expression, decreases expression	2
diallyl trisulfide	decreases expression, increases expression	2
3-(4-methylphenylsulfonyl)-2-propenenitrile	decreases expression	2
NVP-BKM120	affects cotreatment, decreases expression	2
Wortmannin	decreases reaction, increases expression, decreases expression	2
Zoledronic Acid	affects cotreatment, decreases expression	2
Vorinostat	affects cotreatment, decreases expression, decreases reaction, increases expression	2
Air Pollutants	decreases expression, increases abundance, increases expression	2
Dexamethasone	affects cotreatment, increases expression, decreases expression, decreases reaction	2
Estradiol	affects expression, decreases expression	2
Aflatoxin B1	decreases methylation, increases expression	2
Etodolac	decreases expression, increases activity	2
Reactive Oxygen Species	decreases expression, increases chemical synthesis, increases abundance	2
aristolochic acid I	decreases expression	1
1-hydroxyalantolactone	decreases activity	1
bisphenol F	affects cotreatment, increases expression	1

ChEMBL screening assays

297 unique, capped per target: 294 binding, 3 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2182118	Binding	Binding affinity to Flag-tagged cIAP1/CRABP2 expressed in human IMR32 cells assessed as reduction in MycN level at 1 to 10 uM after 48 hrs by Western blot analysis	Development of target protein-selective degradation inducer for protein knockdown. — Bioorg Med Chem
CHEMBL1952922	Functional	Antagonist activity at GST-tagged BIR3 domain of cIAP1 using AbuRPFK-5FAM after 20 mins by fluorescence polarization assay	Discovery of aminopiperidine-based Smac mimetics as IAP antagonists. — Bioorg Med Chem Lett

Cellosaurus cell lines

5 cell lines: 5 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B1L9	Abcam HeLa BIRC2 KO	Cancer cell line	Female
CVCL_D7L0	Ubigene A-549 BIRC2 KO	Cancer cell line	Male
CVCL_D9YM	Ubigene HeLa BIRC2 KO	Cancer cell line	Female
CVCL_SF16	HAP1 BIRC2 (-) 1	Cancer cell line	Male
CVCL_SF17	HAP1 BIRC2 (-) 2	Cancer cell line	Male

Clinical trials (associated diseases)

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