Page last updated: 2024-11-11

pd 90780

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

PD 90780: a nonpeptide inhibitor of nerve growth factor; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9885305
CHEMBL ID137953
SCHEMBL ID2727308
MeSH IDM0254622

Synonyms (22)

Synonym
bdbm50029495
7-benzoylamino-4-methyl-9-oxo-4,9-dihydro-pyrazolo[5,1-b]quinazoline-2-carboxylic acid
CHEMBL137953 ,
pd 90780
SCHEMBL2727308
IAZAGXDMMVWYKF-UHFFFAOYSA-N ,
7-(benzoylamino)-4,9-dihydro-4-methyl-9-oxopyrazolo-[5,1-b]quinazoline-2-carboxylic acid
AKOS025142048
7-(benzoylamino)-4,9-dihydro-4-methyl-9-oxo-pyrazolo[5,1-b]quinazoline-2-carboxylic acid
77422-99-2
pd90780
7-benzamido-4-methyl-9-oxo-4,9-dihydropyrazolo[5,1-b]quinazoline-2-carboxylic acid
NCGC00386708-02
pd-90780;pd 90780
BCP16228
HY-110166
7-benzamido-4-methyl-9-oxopyrazolo[5,1-b]quinazoline-2-carboxylic acid
CS-0033028
MS-25748
NCGC00386708-01
CDA42299
E98677

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
High affinity nerve growth factor receptorHomo sapiens (human)IC50 (µMol)47.00000.00020.543610.0000AID1322459
Tumor necrosis factor receptor superfamily member 16Homo sapiens (human)IC50 (µMol)55.10000.20001.96003.7200AID1322457; AID147189
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (69)

Processvia Protein(s)Taxonomy
cellular response to amyloid-betaHigh affinity nerve growth factor receptorHomo sapiens (human)
positive regulation of protein phosphorylationHigh affinity nerve growth factor receptorHomo sapiens (human)
protein phosphorylationHigh affinity nerve growth factor receptorHomo sapiens (human)
axon guidanceHigh affinity nerve growth factor receptorHomo sapiens (human)
learning or memoryHigh affinity nerve growth factor receptorHomo sapiens (human)
circadian rhythmHigh affinity nerve growth factor receptorHomo sapiens (human)
negative regulation of cell population proliferationHigh affinity nerve growth factor receptorHomo sapiens (human)
response to xenobiotic stimulusHigh affinity nerve growth factor receptorHomo sapiens (human)
programmed cell death involved in cell developmentHigh affinity nerve growth factor receptorHomo sapiens (human)
positive regulation of neuron projection developmentHigh affinity nerve growth factor receptorHomo sapiens (human)
peptidyl-tyrosine phosphorylationHigh affinity nerve growth factor receptorHomo sapiens (human)
olfactory nerve developmentHigh affinity nerve growth factor receptorHomo sapiens (human)
B cell differentiationHigh affinity nerve growth factor receptorHomo sapiens (human)
response to nutrient levelsHigh affinity nerve growth factor receptorHomo sapiens (human)
peptidyl-tyrosine autophosphorylationHigh affinity nerve growth factor receptorHomo sapiens (human)
nerve growth factor signaling pathwayHigh affinity nerve growth factor receptorHomo sapiens (human)
mechanoreceptor differentiationHigh affinity nerve growth factor receptorHomo sapiens (human)
negative regulation of apoptotic processHigh affinity nerve growth factor receptorHomo sapiens (human)
positive regulation of programmed cell deathHigh affinity nerve growth factor receptorHomo sapiens (human)
negative regulation of neuron apoptotic processHigh affinity nerve growth factor receptorHomo sapiens (human)
positive regulation of GTPase activityHigh affinity nerve growth factor receptorHomo sapiens (human)
positive regulation of Ras protein signal transductionHigh affinity nerve growth factor receptorHomo sapiens (human)
protein autophosphorylationHigh affinity nerve growth factor receptorHomo sapiens (human)
neurotrophin TRK receptor signaling pathwayHigh affinity nerve growth factor receptorHomo sapiens (human)
ephrin receptor signaling pathwayHigh affinity nerve growth factor receptorHomo sapiens (human)
sympathetic nervous system developmentHigh affinity nerve growth factor receptorHomo sapiens (human)
response to axon injuryHigh affinity nerve growth factor receptorHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of painHigh affinity nerve growth factor receptorHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painHigh affinity nerve growth factor receptorHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityHigh affinity nerve growth factor receptorHomo sapiens (human)
neuron apoptotic processHigh affinity nerve growth factor receptorHomo sapiens (human)
response to hydrostatic pressureHigh affinity nerve growth factor receptorHomo sapiens (human)
response to electrical stimulusHigh affinity nerve growth factor receptorHomo sapiens (human)
positive regulation of synapse assemblyHigh affinity nerve growth factor receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicHigh affinity nerve growth factor receptorHomo sapiens (human)
Sertoli cell developmentHigh affinity nerve growth factor receptorHomo sapiens (human)
axonogenesis involved in innervationHigh affinity nerve growth factor receptorHomo sapiens (human)
behavioral response to formalin induced painHigh affinity nerve growth factor receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeHigh affinity nerve growth factor receptorHomo sapiens (human)
cellular response to nicotineHigh affinity nerve growth factor receptorHomo sapiens (human)
cellular response to nerve growth factor stimulusHigh affinity nerve growth factor receptorHomo sapiens (human)
multicellular organism developmentHigh affinity nerve growth factor receptorHomo sapiens (human)
positive regulation of kinase activityHigh affinity nerve growth factor receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayHigh affinity nerve growth factor receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeHigh affinity nerve growth factor receptorHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionHigh affinity nerve growth factor receptorHomo sapiens (human)
intracellular glucose homeostasisTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
intracellular protein transportTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
Rho protein signal transductionTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
axon guidanceTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
central nervous system developmentTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
fibroblast growth factor receptor signaling pathwayTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
detection of temperature stimulusTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
nerve developmentTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
negative regulation of cell migrationTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
hair follicle morphogenesisTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
circadian regulation of gene expressionTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
dorsal aorta developmentTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
negative regulation of fibroblast growth factor receptor signaling pathwayTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
odontogenesis of dentin-containing toothTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
positive regulation of odontogenesis of dentin-containing toothTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
glucose homeostasisTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
fibroblast proliferationTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
positive regulation of fibroblast proliferationTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
neuron apoptotic processTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
negative regulation of hair follicle developmentTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
positive regulation of protein localization to nucleusTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
positive regulation of miRNA transcriptionTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
negative regulation of blood vessel endothelial cell proliferation involved in sprouting angiogenesisTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
positive regulation of apoptotic signaling pathwayTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
protein tyrosine kinase activityHigh affinity nerve growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityHigh affinity nerve growth factor receptorHomo sapiens (human)
GPI-linked ephrin receptor activityHigh affinity nerve growth factor receptorHomo sapiens (human)
neurotrophin p75 receptor bindingHigh affinity nerve growth factor receptorHomo sapiens (human)
protein bindingHigh affinity nerve growth factor receptorHomo sapiens (human)
ATP bindingHigh affinity nerve growth factor receptorHomo sapiens (human)
nerve growth factor receptor activityHigh affinity nerve growth factor receptorHomo sapiens (human)
kinase bindingHigh affinity nerve growth factor receptorHomo sapiens (human)
identical protein bindingHigh affinity nerve growth factor receptorHomo sapiens (human)
protein homodimerization activityHigh affinity nerve growth factor receptorHomo sapiens (human)
nerve growth factor bindingHigh affinity nerve growth factor receptorHomo sapiens (human)
neurotrophin bindingHigh affinity nerve growth factor receptorHomo sapiens (human)
neurotrophin receptor activityHigh affinity nerve growth factor receptorHomo sapiens (human)
amyloid-beta bindingTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
transmembrane signaling receptor activityTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
death receptor activityTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
protein bindingTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
calmodulin bindingTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
coreceptor activityTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
small GTPase bindingTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
ubiquitin protein ligase bindingTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
signaling receptor activityTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
neurotrophin bindingTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
nerve growth factor bindingTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
early endosomeHigh affinity nerve growth factor receptorHomo sapiens (human)
late endosomeHigh affinity nerve growth factor receptorHomo sapiens (human)
plasma membraneHigh affinity nerve growth factor receptorHomo sapiens (human)
cell surfaceHigh affinity nerve growth factor receptorHomo sapiens (human)
endosome membraneHigh affinity nerve growth factor receptorHomo sapiens (human)
dendriteHigh affinity nerve growth factor receptorHomo sapiens (human)
early endosome membraneHigh affinity nerve growth factor receptorHomo sapiens (human)
late endosome membraneHigh affinity nerve growth factor receptorHomo sapiens (human)
neuronal cell bodyHigh affinity nerve growth factor receptorHomo sapiens (human)
recycling endosome membraneHigh affinity nerve growth factor receptorHomo sapiens (human)
protein-containing complexHigh affinity nerve growth factor receptorHomo sapiens (human)
receptor complexHigh affinity nerve growth factor receptorHomo sapiens (human)
axonHigh affinity nerve growth factor receptorHomo sapiens (human)
plasma membraneHigh affinity nerve growth factor receptorHomo sapiens (human)
extracellular regionTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
nucleoplasmTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
endosomeTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
cytosolTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
plasma membraneTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
cell-cell junctionTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
cell surfaceTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
postsynaptic densityTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
membraneTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
growth coneTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
neuromuscular junctionTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
dendritic spineTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
perikaryonTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
presynapseTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
plasma membraneTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
cell surfaceTumor necrosis factor receptor superfamily member 16Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (12)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1322458Inhibition of mouse NGF binding to p75 (unknown origin) by SPR method relative to control2017Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
Targeting the Nerve Growth Factor (NGF) Pathway in Drug Discovery. Potential Applications to New Therapies for Chronic Pain.
AID182690Inhibition of passive cutaneous anaphylaxis (PCA) reaction in rats by intraperitoneal administration of 5 mg/kg1981Journal of medicinal chemistry, Jun, Volume: 24, Issue:6
Pyrazolo[5,1-b]quinazolin-9-ones: a new series of antiallergic agents.
AID1322460Inhibition of mouse NGF binding to TrkA (unknown origin) by SPR method relative to control2017Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
Targeting the Nerve Growth Factor (NGF) Pathway in Drug Discovery. Potential Applications to New Therapies for Chronic Pain.
AID1322457Inhibition of mouse NGF binding to p75 (unknown origin) by SPR method2017Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
Targeting the Nerve Growth Factor (NGF) Pathway in Drug Discovery. Potential Applications to New Therapies for Chronic Pain.
AID182824Inhibition of passive cutaneous anaphylaxis (PCA) reaction in rats, peroral administration 5 mg/kg1981Journal of medicinal chemistry, Jun, Volume: 24, Issue:6
Pyrazolo[5,1-b]quinazolin-9-ones: a new series of antiallergic agents.
AID1322459Inhibition of mouse NGF binding to TrkA (unknown origin) by SPR method2017Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
Targeting the Nerve Growth Factor (NGF) Pathway in Drug Discovery. Potential Applications to New Therapies for Chronic Pain.
AID147189Inhibition of [125I]- NGF binding to extracellular domain of p75 receptor1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
Kynurenic acid derivatives inhibit the binding of nerve growth factor (NGF) to the low-affinity p75 NGF receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (7.14)18.7374
1990's2 (14.29)18.2507
2000's4 (28.57)29.6817
2010's5 (35.71)24.3611
2020's2 (14.29)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.23

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.23 (24.57)
Research Supply Index2.71 (2.92)
Research Growth Index4.93 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.23)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (7.14%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (92.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]