gdc-0152 profile

GDC-0152: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	46940575
CHEMBL ID	2063869
SCHEMBL ID	10166489
MeSH ID	M0582275

Synonym
bdbm50388975
873652-48-3
gdc-0152
CHEMBL2063869 ,
(2s)-1-[(2s)-2-cyclohexyl-2-[[(2s)-2-(methylamino)propanoyl]amino]acetyl]-n-(4-phenylthiadiazol-5-yl)pyrrolidine-2-carboxamide
gdc0152
gtpl7733
gdc 0152
4kw1m48shs ,
unii-4kw1m48shs
l-prolinamide, n-methyl-l-alanyl-(2s)-2-cyclohexylglycyl-n-(4-phenyl-1,2,3-thiadiazol-5-yl)-
CS-3546
SCHEMBL10166489
HY-13638
AC-32972
DTXSID00236307
(s)-1-((s)-2-cyclohexyl-2-((s)-2-(methylamino)propanamido)acetyl)-n-(4-phenyl-1,2,3-thiadiazol-5-yl)pyrrolidine-2-carboxamide
SW220303-1
DB12380
gdc-0152 free base
873652-48-3 (free base)
Z2235802113
S7010
EX-A1658
Q27077778
WZRFLSDVFPIXOV-LRQRDZAKSA-N ,
CCG-269679
D71050
A916910
GS-9762
(2s)-1-[(2s)-2-cyclohexyl-2-[(2s)-2-(methylamino)propanamido]acetyl]-n-(4-phenyl-1,2,3-thiadiazol-5-yl)pyrrolidine-2-carboxamide
nsc765898
nsc-765898
AKOS040758990

Excerpt	Relevance	Reference
" Compound 1 inhibits tumor growth when dosed orally in the MDA-MB-231 breast cancer xenograft model."	( Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152). Beresini, M; Budha, N; Chan, H; Chan, IT; Cheeti, S; Cohen, F; Deshayes, K; Doerner, K; Eckhardt, SG; Elliott, LO; Fairbrother, WJ; Feng, B; Flygare, JA; Franklin, MC; Gazzard, L; Halladay, J; Hymowitz, SG; La, H; LoRusso, P; Maurer, B; Murray, L; Plise, E; Quan, C; Reisner, SF; Stephan, JP; Tom, J; Tsui, V; Um, J; Varfolomeev, E; Vucic, D; Wagner, AJ; Wallweber, HJ; Wang, L; Ware, J; Wen, Z; Wong, H; Wong, JM; Wong, M; Wong, S; Young, SG; Yu, R; Zobel, K, 2012)	0.58

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)	IC50 (µMol)	0.0316	0.0075	0.6227	4.1000	AID1410827; AID1509247; AID1509248
E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)	Ki	7.5500	0.0020	0.1067	0.4000	AID676461; AID676462; AID758066; AID758067
Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)	IC50 (µMol)	0.0129	0.0085	0.0893	0.6900	AID1410829
Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)	Ki	4.8215	0.0020	1.9304	9.6000	AID676464; AID676466
Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)	IC50 (µMol)	0.0104	0.0004	0.3121	2.7200	AID1410828
Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)	Ki	7.2585	0.0005	0.0044	0.0170	AID676463; AID676465
Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)	Ki	0.0500	0.0500	0.0500	0.0500	AID676460
Max-like protein X	Homo sapiens (human)	Ki	0.0140	0.0140	0.0140	0.0140	AID676467
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)	Kd	0.0760	0.0280	0.2051	0.9000	AID1410826; AID1553566; AID1553573
Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)	Kd	0.0430	0.0129	0.0306	0.0430	AID1553575
Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)	Kd	0.0170	0.0010	0.0095	0.0170	AID1553574
Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)	Kd	0.0140	0.0010	0.0075	0.0140	AID1553576
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
regulation of apoptotic process	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
DNA damage response	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
negative regulation of tumor necrosis factor-mediated signaling pathway	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
Wnt signaling pathway	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
regulation of BMP signaling pathway	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
positive regulation of protein ubiquitination	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
positive regulation of type I interferon production	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
regulation of cell population proliferation	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
defense response to bacterium	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
negative regulation of apoptotic process	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic process	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
regulation of innate immune response	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
positive regulation of JNK cascade	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
regulation of inflammatory response	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
neuron apoptotic process	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
copper ion homeostasis	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
regulation of apoptosis involved in tissue homeostasis	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
regulation of nucleotide-binding domain, leucine rich repeat containing receptor signaling pathway	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
nucleotide-binding oligomerization domain containing 1 signaling pathway	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
nucleotide-binding oligomerization domain containing 2 signaling pathway	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
protein K63-linked ubiquitination	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
positive regulation of canonical Wnt signaling pathway	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
inhibition of cysteine-type endopeptidase activity	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
positive regulation of protein linear polyubiquitination	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
regulation of cell cycle	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
apoptotic process	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
cell surface receptor signaling pathway	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
canonical NF-kappaB signal transduction	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
spermatogenesis	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
positive regulation of protein ubiquitination	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
tumor necrosis factor-mediated signaling pathway	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
regulation of toll-like receptor signaling pathway	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
non-canonical NF-kappaB signal transduction	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
regulation of RIG-I signaling pathway	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
regulation of apoptotic process	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
regulation of innate immune response	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
regulation of inflammatory response	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
regulation of necroptotic process	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
regulation of nucleotide-binding domain, leucine rich repeat containing receptor signaling pathway	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
regulation of cysteine-type endopeptidase activity	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
regulation of cell cycle	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
negative regulation of apoptotic process	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
negative regulation of necroptotic process	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
protein polyubiquitination	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
response to hypoxia	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
placenta development	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
apoptotic process	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
cell surface receptor signaling pathway	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
canonical NF-kappaB signal transduction	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
tumor necrosis factor-mediated signaling pathway	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
regulation of toll-like receptor signaling pathway	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
non-canonical NF-kappaB signal transduction	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
regulation of RIG-I signaling pathway	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
regulation of cell population proliferation	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
regulation of apoptotic process	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
negative regulation of apoptotic process	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic process	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
regulation of innate immune response	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
response to ethanol	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
regulation of cell differentiation	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
positive regulation of DNA-templated transcription	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
regulation of inflammatory response	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
response to cAMP	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
regulation of cell cycle	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
regulation of necroptotic process	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
necroptotic process	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
regulation of nucleotide-binding domain, leucine rich repeat containing receptor signaling pathway	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
regulation of non-canonical NF-kappaB signal transduction	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
negative regulation of ripoptosome assembly involved in necroptotic process	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
positive regulation of protein K63-linked ubiquitination	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
positive regulation of protein K48-linked ubiquitination	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
positive regulation of protein monoubiquitination	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
regulation of cysteine-type endopeptidase activity	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
regulation of reactive oxygen species metabolic process	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
positive regulation of protein ubiquitination	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
negative regulation of necroptotic process	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
regulation of apoptotic process	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
lens development in camera-type eye	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
apoptotic process	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
negative regulation of tumor necrosis factor-mediated signaling pathway	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
protein ubiquitination	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
regulation of cell population proliferation	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
negative regulation of apoptotic process	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
positive regulation of JNK cascade	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
regulation of natural killer cell apoptotic process	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
positive regulation of protein ubiquitination	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
regulation of cell cycle	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Max-like protein X	Homo sapiens (human)
regulation of DNA-templated transcription	Max-like protein X	Homo sapiens (human)
negative regulation of DNA-templated transcription	Max-like protein X	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Max-like protein X	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Max-like protein X	Homo sapiens (human)
positive regulation of cellular metabolic process	Max-like protein X	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
ubiquitin-protein transferase activity	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
cysteine-type endopeptidase inhibitor activity	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
protein binding	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
identical protein binding	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic process	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
metal ion binding	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
endopeptidase regulator activity	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
ubiquitin protein ligase activity	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
protein serine/threonine kinase binding	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
ubiquitin-protein transferase activity	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
protein binding	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
transferase activity	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
protein-containing complex binding	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
metal ion binding	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic process	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
ubiquitin protein ligase activity	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
transcription coactivator activity	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
ubiquitin-protein transferase activity	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
protein binding	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
zinc ion binding	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
transferase activity	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
identical protein binding	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
ubiquitin binding	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
protein-containing complex binding	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
protein-folding chaperone binding	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
FBXO family protein binding	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
ubiquitin protein ligase activity	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic process	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
ubiquitin-protein transferase activity	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
cysteine-type endopeptidase inhibitor activity	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
protein binding	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
enzyme binding	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
metal ion binding	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic process	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
ubiquitin protein ligase activity	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA binding	Max-like protein X	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Max-like protein X	Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specific	Max-like protein X	Homo sapiens (human)
DNA binding	Max-like protein X	Homo sapiens (human)
DNA-binding transcription factor activity	Max-like protein X	Homo sapiens (human)
protein binding	Max-like protein X	Homo sapiens (human)
protein homodimerization activity	Max-like protein X	Homo sapiens (human)
protein heterodimerization activity	Max-like protein X	Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor binding	Max-like protein X	Homo sapiens (human)
sequence-specific double-stranded DNA binding	Max-like protein X	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Max-like protein X	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Max-like protein X	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
cytoplasm	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
nucleus	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
nucleoplasm	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
cytoplasm	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
cytosol	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
nucleus	E3 ubiquitin-protein ligase XIAP	Homo sapiens (human)
nucleus	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
nucleoplasm	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
cytoplasm	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
cytosol	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
protein-containing complex	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
nucleus	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
cytoplasm	Baculoviral IAP repeat-containing protein 3	Homo sapiens (human)
XY body	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
nucleus	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
cytoplasm	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
cytosol	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
cytoplasmic side of plasma membrane	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
CD40 receptor complex	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
nucleus	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
cytoplasm	Baculoviral IAP repeat-containing protein 2	Homo sapiens (human)
nucleus	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
nucleoplasm	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
cytoplasm	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
Golgi apparatus	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
centrosome	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
cytosol	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
cytoplasm	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
nucleus	Baculoviral IAP repeat-containing protein 7	Homo sapiens (human)
nucleus	Max-like protein X	Homo sapiens (human)
nucleoplasm	Max-like protein X	Homo sapiens (human)
cytoplasm	Max-like protein X	Homo sapiens (human)
cytosol	Max-like protein X	Homo sapiens (human)
nuclear membrane	Max-like protein X	Homo sapiens (human)
chromatin	Max-like protein X	Homo sapiens (human)
nucleus	Max-like protein X	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (79)

Assay ID	Title	Year	Journal	Article
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID676498	Ratio of drug level in blood to plasma in human by equilibrium dialysis assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1410828	Displacement of AVPIAQKSEK-biotin from cIAP1 BIR3 (unknown origin) after 1 hr by DELFIA	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
AID676471	Inhibition of Flag-tagged XIAP BIR3 domain binding to cIAP2 expressed in human HEK293T cells at 1 to 50 uM after 2 hrs by immunoprecipitation	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID676464	Displacement of 5-FAM-conjugated AVP-diPhe-FAM from cIAP2 BIR3 domain after 30 mins by fluorescence polarization-based competition assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1410834	Antiproliferative activity against human MOLT4 cells after 48 hrs by ATPlite 1Step luminescence assay	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
AID676463	Displacement of 5-FAM-conjugated AVP-diPhe-FAM from cIAP1 BIR3 domain after 30 mins by fluorescence polarization-based competition assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID676496	Ratio of drug level in blood to plasma in dog by equilibrium dialysis assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1553574	Binding affinity to cIAP1-BIR3 domain (unknown origin)	2019	Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12	Inhibitor of Apoptosis Protein (IAP) Antagonists in Anticancer Agent Discovery: Current Status and Perspectives.
AID1410845	Inhibition of cIAP1 in human PANC1 cells assessed as potentiation of gemcitabine induced growth inhibition at 15 uM pretreated with gemcitabine for 24 hrs followed by compound addition and measured after 24 hrs by ATPlite 1Step luminescence assay	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
AID676486	Kinetic solubility of the compound at pH 6.7	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID676481	Induction of proteasomal degradation of cIAP1 in human A2058 cells after 15 mins by immunoblotting	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1196853	Cytotoxicity against XIAP-dependent human A875 cells assessed as cell viability after 72 hrs by MTS assay	2015	Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3	Discovery of potent heterodimeric antagonists of inhibitor of apoptosis proteins (IAPs) with sustained antitumor activity.
AID1553566	Binding affinity to XIAP-BIR3 domain (241 to 356 residues) (unknown origin) by fluorescence polarization-based competition assay	2019	Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12	Inhibitor of Apoptosis Protein (IAP) Antagonists in Anticancer Agent Discovery: Current Status and Perspectives.
AID1410835	Induction of cIAP1 protein degradation in human MOLT4 cells at 1 uM incubated for 3 hrs by Western blot analysis	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
AID1410847	Inhibition of XIAP in human BxPC3 cells assessed as potentiation of gemcitabine induced growth inhibition at 15 uM pretreated with gemcitabine for 24 hrs followed by compound addition and measured after 24 hrs by ATPlite 1Step luminescence assay	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
AID1410827	Displacement of AVPIAQKSEK-biotin from N-terminal His-tagged human recombinant XIAP BIR3 (253 to 347 residues) expressed in Escherichia coli BL21(DE3) Gold after 1 hr by DELFIA	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
AID676488	Plasma protein binding in CD-1 mouse at 0.1 to 100 uM by equilibrium dialysis assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1509251	Covalent binding affinity to N-terminal His tagged recombinant human XIAP-BIR3 domain (253 to 347 residues) expressed in Escherichia coli BL21(DE3) cells assessed as change in melting temperature incubated for 6 hrs by SYPRO orange dye-based thermal shift	2019	Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11	Covalent Inhibitors of Protein-Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues.
AID676468	Inhibition of Flag-tagged XIAP BIR3 domain binding to caspase-9 expressed in human HEK293T cells at 1 to 100 uM after 2 hrs by immunoprecipitation	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID676467	Displacement of 5-FAM-conjugated AVP-diPhe-FAM from MLXBIR3SG after 30 mins by fluorescence polarization-based competition assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1410843	Inhibition of XIAP in human MIAPaCa2 cells assessed as potentiation of gemcitabine induced growth inhibition at 15 uM pretreated with gemcitabine for 24 hrs followed by compound addition and measured after 24 hrs by ATPlite 1Step luminescence assay	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
AID676462	Displacement of 5-FAM-conjugated AVP-diPhe-FAM from XIAP BIR2 domain after 30 mins by fluorescence polarization-based competition assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID676472	Inhibition of ML-IAP binding to Smax expressed in gemcitabine and zVAd treated human SK-MEL28 cells at 0.5 uM by immunoprecipitation	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1509292	Stabilization of N-terminal His tagged recombinant human XIAP-BIR3 domain (253 to 347 residues) expressed in Escherichia coli BL21(DE3) cells cells at 40 uM after 3 hrs by 1H-1D NMR spectra analysis	2019	Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11	Covalent Inhibitors of Protein-Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues.
AID676493	Ratio of drug level in blood to plasma in CD-1 mouse by equilibrium dialysis assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1410848	Inhibition of cIAP1 in human BxPC3 cells assessed as potentiation of gemcitabine induced growth inhibition at 15 uM pretreated with gemcitabine for 24 hrs followed by compound addition and measured after 24 hrs by ATPlite 1Step luminescence assay	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
AID1410846	Inhibition of cIAP2 in human PANC1 cells assessed as potentiation of gemcitabine induced growth inhibition at 15 uM pretreated with gemcitabine for 24 hrs followed by compound addition and measured after 24 hrs by ATPlite 1Step luminescence assay	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
AID676492	Plasma protein binding in human 0.1 to 100 uM by equilibrium dialysis assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID676485	Kinetic solubility of the compound at pH 5.5	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID676474	Cytotoxicity against human HMEC after 72 hrs by CellTiter-Glo luminescent cell viability assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1509295	Induction of apoptosis in human SKOV3 cells assessed caspase-3 activation after 24 hrs by IncuCyte S3 live-cell analysis	2019	Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11	Covalent Inhibitors of Protein-Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues.
AID676476	Induction of apoptosis in human MDA-MB-231 cells assessed as activation of caspase-7 up to 10 uM by Apo-ONE homogenous assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID676487	Kinetic solubility of the compound at pH 7.7	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID676466	Displacement of AVPFAK(5-FAM)K (Hid-FAM) from cIAP2 BIR2 domain after 30 mins by fluorescence polarization-based competition assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID676461	Displacement of 5-FAM-conjugated AVP-diPhe-FAM from XIAP BIR3 domain after 30 mins by fluorescence polarization-based competition assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID676465	Displacement of AVPFAK(5-FAM)K (Hid-FAM) from cIAP1 BIR2 domain after 30 mins by fluorescence polarization-based competition assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID676495	Ratio of drug level in blood to plasma in rabbit by equilibrium dialysis assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1410840	Cytotoxicity against human NCI-H929 cells assessed as decrease in cell viability at 20 uM after 48 hrs by MTS assay	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
AID676473	Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescent assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1509247	Displacement of biotinylated AVPF from N-terminal His tagged recombinant human XIAP-BIR3 domain (253 to 347 residues) expressed in Escherichia coli BL21(DE3) cells incubated for 8 hrs by DELFIA	2019	Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11	Covalent Inhibitors of Protein-Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues.
AID676460	Binding affinity to ML-IAP BIR domain after 30 mins by fluorescence polarization-based competition assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID676469	Inhibition of Flag-tagged XIAP BIR3 domain binding to ML-IAP expressed in human HEK293T cells at 1 to 50 uM after 2 hrs by immunoprecipitation	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID676478	Induction of apoptosis in human MDA-MB-231 cells assessed as activation of caspase-7 for 3 to 24 hrs by Apo-ONE homogenous assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1410844	Inhibition of XIAP in human PANC1 cells assessed as potentiation of gemcitabine induced growth inhibition at 15 uM pretreated with gemcitabine for 24 hrs followed by compound addition and measured after 24 hrs by ATPlite 1Step luminescence assay	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
AID676489	Plasma protein binding in rat 0.1 to 100 uM by equilibrium dialysis assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID676497	Ratio of drug level in blood to plasma in monkey by equilibrium dialysis assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID676470	Inhibition of Flag-tagged XIAP BIR3 domain binding to cIAP1 expressed in human HEK293T cells at 1 to 50 uM after 2 hrs by immunoprecipitation	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1410849	Inhibition of cIAP2 in human BxPC3 cells assessed as potentiation of gemcitabine induced growth inhibition at 15 uM pretreated with gemcitabine for 24 hrs followed by compound addition and measured after 24 hrs by ATPlite 1Step luminescence assay	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
AID674066	Apparent permeability from apical to basal side of MDCK cells	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID758064	Selectivity ratio of Ki for XIAP-BIR2 domain (unknown origin) to Ki for XIAP-BIR3 domain (unknown origin)	2013	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14	Design, synthesis and evaluation of inhibitor of apoptosis protein (IAP) antagonists that are highly selective for the BIR2 domain of XIAP.
AID1509246	Binding affinity to N-terminal human XIAP-BIR3 domain (262 to 350 residues) expressed in HEK293 cells assessed as covalent adduct formation at 10 uM incubated for 6 hrs by Coomassie blue staining-based SDS-PAGE analysis	2019	Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11	Covalent Inhibitors of Protein-Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues.
AID676459	Plasma protein binding in rabbit 0.1 to 100 uM by equilibrium dialysis assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID674059	Volume of distribution in human with locally advanced or metastatic solid malignancies or non Hodgkin's lymphoma with out leukemic phase at 0.049 to 1.48 mg/kg, iv administered as 0.5 hr infusion every 14 days	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID758066	Competitive inhibition of XIAP-BIR3 domain (unknown origin) by fluorescence polarization assay	2013	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14	Design, synthesis and evaluation of inhibitor of apoptosis protein (IAP) antagonists that are highly selective for the BIR2 domain of XIAP.
AID1410829	Displacement of AVPIAQKSEK-biotin from cIAP2 BIR3 (unknown origin) after 1 hr by DELFIA	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
AID1509293	Permeability in HEK293 cells expressing human N-terminal XIAP-BIR3 domain (262 to 350 residues) at 10 uM incubated for 6 hrs by Coomassie blue staining-based SDS-PAGE analysis	2019	Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11	Covalent Inhibitors of Protein-Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues.
AID676490	Plasma protein binding in dog 0.1 to 100 uM by equilibrium dialysis assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1509250	Covalent binding affinity to N-terminal His tagged recombinant human XIAP-BIR3 domain (253 to 347 residues) expressed in Escherichia coli BL21(DE3) cells assessed as change in melting temperature incubated for 2 hrs by SYPRO orange dye-based thermal shift	2019	Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11	Covalent Inhibitors of Protein-Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues.
AID1509290	Half-life in mouse plasma at 200 uM by LC-MS method	2019	Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11	Covalent Inhibitors of Protein-Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues.
AID674058	Plasma clearance in human with locally advanced or metastatic solid malignancies or non Hodgkin's lymphoma with out leukemic phase at 0.049 to 1.48 mg/kg, iv administered as 0.5 hr infusion every 14 days	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1553576	Binding affinity to ML-IAP-BIR domain (unknown origin)	2019	Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12	Inhibitor of Apoptosis Protein (IAP) Antagonists in Anticancer Agent Discovery: Current Status and Perspectives.
AID1553573	Binding affinity to XIAP-BIR2 domain (unknown origin) by fluorescence polarization-based competition assay	2019	Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12	Inhibitor of Apoptosis Protein (IAP) Antagonists in Anticancer Agent Discovery: Current Status and Perspectives.
AID1410839	Cytotoxicity against human L363 cells assessed as decrease in cell viability at 20 uM after 48 hrs by MTS assay	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
AID676475	Induction of apoptosis in human MDA-MB-231 cells assessed as activation of caspase-3 up to 10 uM by Apo-ONE homogenous assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1509294	Stabilization of N-terminal human XIAP-BIR3 domain (262 to 350 residues) expressed in HEK293 cells assessed as increase in protein band intensity at 10 uM incubated for 6 hrs by Coomassie blue staining-based SDS-PAGE analysis	2019	Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11	Covalent Inhibitors of Protein-Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues.
AID676494	Ratio of drug level in blood to plasma in rat by equilibrium dialysis assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1410836	Induction of cIAP2 protein degradation in human MOLT4 cells at 1 uM incubated for 3 hrs by Western blot analysis	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
AID676491	Plasma protein binding in monkey 0.1 to 100 uM by equilibrium dialysis assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1509248	Displacement of biotinylated AVPF from N-terminal His tagged recombinant human XIAP-BIR3 domain (253 to 347 residues) expressed in Escherichia coli BL21(DE3) cells incubated for 2 hrs by DELFIA	2019	Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11	Covalent Inhibitors of Protein-Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues.
AID1509296	Induction of apoptosis in human SKOV3 cells assessed caspase-3 activation after 48 hrs by IncuCyte S3 live-cell analysis	2019	Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11	Covalent Inhibitors of Protein-Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues.
AID676477	Induction of apoptosis in human MDA-MB-231 cells assessed as activation of caspase-3 for 3 to 24 hrs by Apo-ONE homogenous assay	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID758067	Competitive inhibition of XIAP-BIR2 domain (unknown origin) by fluorescence polarization assay	2013	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14	Design, synthesis and evaluation of inhibitor of apoptosis protein (IAP) antagonists that are highly selective for the BIR2 domain of XIAP.
AID1410826	Binding affinity to N-terminal His-tagged human recombinant XIAP BIR3 (253 to 347 residues) expressed in Escherichia coli BL21(DE3) Gold by isothermal titration calorimetric analysis	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
AID1553575	Binding affinity to cIAP2-BIR3 domain (unknown origin)	2019	Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12	Inhibitor of Apoptosis Protein (IAP) Antagonists in Anticancer Agent Discovery: Current Status and Perspectives.
AID1346249	Human baculoviral IAP repeat containing 2 (Inhibitors of apoptosis (IAP) protein family)	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1346218	Human baculoviral IAP repeat containing 7 (Inhibitors of apoptosis (IAP) protein family)	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1346238	Human baculoviral IAP repeat containing 3 (Inhibitors of apoptosis (IAP) protein family)	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
AID1346157	Human X-linked inhibitor of apoptosis (Inhibitors of apoptosis (IAP) protein family)	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	21 (95.45)	24.3611
2020's	1 (4.55)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	1 (4.55%)	5.53%
Reviews	1 (4.55%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	20 (90.91%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
hippuric acid hippuric acid: RN given refers to parent cpd; structure in Merck Index, 9th ed, #4591. N-benzoylglycine : An N-acylglycine in which the acyl group is specified as benzoyl.	7.08	1	0	N-acylglycine	human blood serum metabolite; uremic toxin
1-aminobenzotriazole [no description available]	2.08	1	0
pyrroles 1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.	6.51	15	1	pyrrole; secondary amine
thiazoles [no description available]	2.57	2	0	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
triazoles Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.	2.51	2	0	1,2,3-triazole
bafilomycin a1 bafilomycin A1: from Streptomyces griseus; structure given in first source. bafilomycin A1 : The most used of the bafilomycins, a family of toxic macrolide antibiotics derived from Streptomyces griseus.	2.17	1	0	cyclic hemiketal; macrolide antibiotic; oxanes	apoptosis inducer; autophagy inhibitor; bacterial metabolite; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor; EC 3.6.3.14 (H(+)-transporting two-sector ATPase) inhibitor; ferroptosis inhibitor; fungicide; potassium ionophore; toxin
sm 164 SM 164: a bivalent Smac mimetic with antineoplastic activity; structure in first source	2.13	1	0	benzenes; organic heterobicyclic compound; secondary carboxamide; triazoles	antineoplastic agent; apoptosis inducer; radiosensitizing agent
lcl161 [no description available]	9.2	4	0	1,3-thiazoles; aromatic ketone; L-alanine derivative; monofluorobenzenes; N-acylpyrrolidine	antineoplastic agent; apoptosis inducer
birinapant birinapant: a Smac mimetic with antineoplastic activity	3.93	3	0	dipeptide
benzyloxycarbonylvalyl-alanyl-aspartyl fluoromethyl ketone benzyloxycarbonylvalyl-alanyl-aspartyl fluoromethyl ketone: an interleukin-1beta converting enzyme (ICE)-like protease inhibitor	2.17	1	0
adrenomedullin Adrenomedullin: A 52-amino acid peptide with multi-functions. It was originally isolated from PHEOCHROMOCYTOMA and ADRENAL MEDULLA but is widely distributed throughout the body including lung and kidney tissues. Besides controlling fluid-electrolyte homeostasis, adrenomedullin is a potent vasodilator and can inhibit pituitary ACTH secretion.	2.21	1	0

Condition	Indicated	Relationship Strength	Studies	Trials
Breast Cancer [description not available]	0	2.07	1	0
Breast Neoplasms Tumors or cancer of the human BREAST.	0	2.07	1	0
Experimental Neoplasms [description not available]	0	2.11	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.21	1	0
Benign Neoplasms [description not available]	0	5.14	3	1
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	1	7.14	3	1
Acute Promyelocytic Leukemia [description not available]	0	2.21	1	0
Leukemia, Promyelocytic, Acute An acute myeloid leukemia in which abnormal PROMYELOCYTES predominate. It is frequently associated with DISSEMINATED INTRAVASCULAR COAGULATION.	0	2.21	1	0
Extravascular Hemolysis [description not available]	0	2.21	1	0
Hemolysis The destruction of ERYTHROCYTES by many different causal agents such as antibodies, bacteria, chemicals, temperature, and changes in tonicity.	0	2.21	1	0
Benign Neoplasms, Brain [description not available]	0	2.21	1	0
Astrocytoma, Grade IV [description not available]	0	2.57	2	0
Brain Neoplasms Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.	0	2.21	1	0
Glioblastoma A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.	0	7.57	2	0
Leucocythaemia [description not available]	0	2.11	1	0
Leukemia A progressive, malignant disease of the blood-forming organs, characterized by distorted proliferation and development of leukocytes and their precursors in the blood and bone marrow. Leukemias were originally termed acute or chronic based on life expectancy but now are classified according to cellular maturity. Acute leukemias consist of predominately immature cells; chronic leukemias are composed of more mature cells. (From The Merck Manual, 2006)	0	7.11	1	0
Bone Cancer [description not available]	0	2.52	2	0
Osteogenic Sarcoma [description not available]	0	2.52	2	0
Bone Neoplasms Tumors or cancer located in bone tissue or specific BONES.	0	2.52	2	0
Osteosarcoma A sarcoma originating in bone-forming cells, affecting the ends of long bones. It is the most common and most malignant of sarcomas of the bones, and occurs chiefly among 10- to 25-year-old youths. (From Stedman, 25th ed)	0	7.52	2	0
Genetic Predisposition [description not available]	0	2.13	1	0
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	0	4.39	1	1
Inflammatory Response Syndrome, Systemic [description not available]	0	2.08	1	0
Systemic Inflammatory Response Syndrome A systemic inflammatory response to a variety of clinical insults, characterized by two or more of the following conditions: (1) fever	0	2.08	1	0

gdc-0152

Description

Cross-References

Synonyms (34)

Research Excerpts

Dosage Studied

Protein Targets (5)

Inhibition Measurements

Activation Measurements

Biological Processes (61)

Molecular Functions (28)

Ceullar Components (12)

Bioassays (79)

Research

Studies (22)

Market Indicators

Research Demand Index: 21.91

Study Types

gdc-0152

Description

Cross-References

Synonyms (34)

Research Excerpts

Dosage Studied

Protein Targets (5)

Inhibition Measurements

Activation Measurements

Biological Processes (61)

Molecular Functions (28)

Ceullar Components (12)

Bioassays (79)

Research

Studies (22)

Market Indicators

Research Demand Index: 21.91

Study Types

Related Drugs (11)

Related Conditions (24)