pf-3893787 profile

PF-3893787: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	24745335
CHEMBL ID	1915540
SCHEMBL ID	12604990
MeSH ID	M0570250

Synonym
nvp-zpl389-nx
zpl-3893787
CHEMBL1915540 ,
pf-3893787
adriforant
zpl-389-nx
pf-03893787
zpl389-nx
zpl-389
bdbm50356884
SCHEMBL12604990
gtpl8985
pf 3893787
zpl3893787
zpl389
n'-(cyclopropylmethyl)-6-[(3r)-3-methylaminopyrrolidin-1-yl]pyrimidine-2,4-diamine
d65h9ye9vu ,
2,4-pyrimidinediamine, n4-(cyclopropylmethyl)-6-((3r)-3-(methylamino)-1-pyrrolidinyl)-
943057-12-3
who 10855
adriforant [usan]
unii-d65h9ye9vu
adriforant [inn]
n4-(cyclopropylmethyl)-6-[(3r)-3-(methylamino)pyrrolidin-1-yl]pyrimidine-2,4-diamine
adriforant [who-dd]
BCP23584
DB15027
Q27089302
EX-A7358
4-n-(cyclopropylmethyl)-6-[(3r)-3-(methylamino)pyrrolidin-1-yl]pyrimidine-2,4-diamine
(r)-n4-(cyclopropylmethyl)-6-(3-(methylamino)pyrrolidin-1-yl)pyrimidine-2,4-diamine

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	Ki	3.4674	0.0021	1.8407	10.0000	AID745212
Histamine H4 receptor	Rattus norvegicus (Norway rat)	Ki	0.0265	0.0024	0.9296	8.5110	AID1249568; AID627801; AID745207
Histamine H4 receptor	Mus musculus (house mouse)	Ki	0.0322	0.0026	0.6978	5.1250	AID1249569; AID627802; AID745206
Histamine H4 receptor	Cavia porcellus (domestic guinea pig)	Ki	0.1230	0.0060	0.3309	1.0715	AID1249567; AID627800
Histamine H4 receptor	Homo sapiens (human)	IC50 (µMol)	0.0181	0.0007	0.6305	10.0000	AID627793; AID627794; AID627795; AID627796; AID745205
Histamine H4 receptor	Homo sapiens (human)	Ki	0.0048	0.0006	0.4787	10.0000	AID1249560; AID1249564; AID627669; AID627670; AID627797; AID745215
Histamine H3 receptor	Homo sapiens (human)	Ki	0.1862	0.0001	0.3399	8.5110	AID745214
[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)
Histamine H4 receptor	Homo sapiens (human)	Kd	0.0251	0.0040	0.0194	0.0702	AID745204
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by hormone	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of DNA-templated transcription	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion homeostasis	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cardiac muscle contraction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cellular response to xenobiotic stimulus	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane depolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion import across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inflammatory response	Histamine H4 receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Histamine H4 receptor	Homo sapiens (human)
biological_process	Histamine H4 receptor	Homo sapiens (human)
regulation of MAPK cascade	Histamine H4 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	Histamine H4 receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	Histamine H4 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Histamine H4 receptor	Homo sapiens (human)
chemical synaptic transmission	Histamine H4 receptor	Homo sapiens (human)
neurotransmitter secretion	Histamine H3 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	Histamine H3 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Histamine H3 receptor	Homo sapiens (human)
chemical synaptic transmission	Histamine H3 receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	Histamine H3 receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
transcription cis-regulatory region binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ubiquitin protein ligase binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
identical protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein homodimerization activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
C3HC4-type RING finger domain binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
scaffold protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
histamine receptor activity	Histamine H4 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor activity	Histamine H4 receptor	Homo sapiens (human)
G protein-coupled acetylcholine receptor activity	Histamine H4 receptor	Homo sapiens (human)
histamine receptor activity	Histamine H3 receptor	Homo sapiens (human)
G protein-coupled acetylcholine receptor activity	Histamine H3 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor activity	Histamine H3 receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cell surface	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
perinuclear region of cytoplasm	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Histamine H4 receptor	Homo sapiens (human)
plasma membrane	Histamine H4 receptor	Homo sapiens (human)
dendrite	Histamine H4 receptor	Homo sapiens (human)
synapse	Histamine H4 receptor	Homo sapiens (human)
plasma membrane	Histamine H3 receptor	Homo sapiens (human)
presynapse	Histamine H3 receptor	Homo sapiens (human)
plasma membrane	Histamine H3 receptor	Homo sapiens (human)
synapse	Histamine H3 receptor	Homo sapiens (human)
dendrite	Histamine H3 receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (56)

Assay ID	Title	Year	Journal	Article
AID627671	Lipophilicity, log D of the compound	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627792	Ratio of drug level in blood to plasma in human	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627984	Inverse agonist activity at macaque H4R expressed in HEK293T cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID1249566	Displacement of [3H]histamine from dog histamine H4 receptor expressed in HEK293T cells	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.
AID627783	Blood clearance in rat at 1 mg/kg, iv and 5 mg/kg, po	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID1249568	Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cells	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.
AID627986	Antagonist activity at dog H4R expressed in HEK293T cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627997	Metabolic stability in rat liver microsomes	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627800	Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627794	Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627780	Volume of distribution in dog blood at 1 mg/kg, iv and 10 mg/kg, po	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627790	Ratio of drug level in blood to plasma in rat at 1 mg/kg, iv and 5 mg/kg, po	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627801	Displacement of [3H]-histamine from rat H4R expressed in HEK293T cells	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627795	Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627803	Inverse agonist activity at human H4R expressed in HEK293T cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627996	Metabolic stability in human liver microsomes	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID745205	Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding	2013	Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9	A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.
AID745211	Displacement of [3H]histamine from human histamine H1 receptor expressed in HEK cells	2013	Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9	A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.
AID627669	Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cells	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID1249569	Displacement of [3H]histamine from mouse histamine H4 receptor expressed in HEK293T cells	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.
AID627789	Plasma protein binding in human	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627990	Partial agonist activity at rat H4R expressed in HEK293T cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID1249560	Binding affinity to human histamine H4 receptor	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.
AID627798	Displacement of [3H]-histamine from macaque H4R expressed in HEK293T cells	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID745209	Selectivity ratio of Ki for human histamine H1 receptor to Ki for human histamine H4 receptor	2013	Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9	A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.
AID745206	Binding affinity to mouse histamine H4 receptor	2013	Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9	A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.
AID745204	Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis	2013	Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9	A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.
AID627782	Oral bioavailability in dog at 10 mg/kg	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627784	Volume of distribution in rat blood at 1 mg/kg, iv and 5 mg/kg, po	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627992	Partial agonist activity at mouse H4R expressed in HEK293T cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID1249564	Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.
AID745214	Displacement of [3H]histamine from human histamine H3 receptor expressed in HEK cells	2013	Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9	A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.
AID745212	Displacement of [3H]astemizole from human ERG channel	2013	Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9	A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.
AID627799	Displacement of [3H]-histamine from dog H4R expressed in HEK293T cells	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID745210	Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells	2013	Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9	A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.
AID627802	Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cells	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID1249565	Displacement of [3H]histamine from monkey histamine H4 receptor expressed in HEK293T cells	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.
AID745213	Selectivity ratio of Ki for human histamine H3 receptor to Ki for human histamine H4 receptor	2013	Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9	A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.
AID627793	Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627670	Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID745215	Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells	2013	Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9	A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.
AID627988	Partial agonist activity at guinea pig H4R expressed in HEK293T cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627779	Blood clearance in dog at 1 mg/kg, iv and 10 mg/kg, po	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627785	Half life in rat at 1 mg/kg, iv and 5 mg/kg, po	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627787	Plasma protein binding in rat at 1 mg/kg, iv and 5 mg/kg, po	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627797	Displacement of [3H]-histamine from human H4R expressed in HEK293T cells	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID745208	Selectivity ratio of Ki for human histamine H2 receptor to Ki for human histamine H4 receptor	2013	Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9	A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.
AID627796	Antagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assay	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627781	Half life in dog at 1 mg/kg, iv and 10 mg/kg, po	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627788	Plasma protein binding in dog at 1 mg/kg, iv and 10 mg/kg, po	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID627791	Ratio of drug level in blood to plasma in dog at 1 mg/kg, iv and 10 mg/kg, po	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID1249567	Displacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cells	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.
AID745207	Binding affinity to rat histamine H4 receptor	2013	Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9	A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.
AID627786	Oral bioavailability in rat at 5 mg/kg	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
AID1346107	Human H3 receptor (Histamine receptors)	2015	Pharmacological reviews, Jul, Volume: 67, Issue:3	International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
AID1346055	Human H4 receptor (Histamine receptors)	2015	Pharmacological reviews, Jul, Volume: 67, Issue:3	International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
[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	6 (100.00)	24.3611
2020's	0 (0.00)	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 (16.67%)	5.53%
Reviews	3 (50.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	2 (33.33%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
histamine [no description available]	3.21	1	aralkylamino compound; imidazoles	human metabolite; mouse metabolite; neurotransmitter
conessine conessine : A steroid alkaloid that is con-5-enine substituted by a N,N-dimethylamino group at position 3. It has been isolated from the plant species of the family Apocynaceae.	3.21	1	steroid alkaloid; tertiary amino compound	antibacterial agent; antimalarial; H3-receptor antagonist; plant metabolite
jnj 7777120 1-((5-chloro-1H-indol-2-yl)carbonyl)-4-methylpiperazine: an H4 receptor antagonist; structure in first source	3.87	3
ciproxifan [no description available]	3.21	1	aromatic ketone
pitolisant pitolisant: functions as both inverse agonist and antagonist of histamine H3 receptors; structure in first source	3.21	1	organochlorine compound
mk-0249 MK-0249: a histamine-3 receptor inverse agonist; structure in first source	3.21	1

Condition	Indicated	Relationship Strength	Studies	Trials
Rheumatoid Arthritis [description not available]	0	3.03	1	0
Asthma, Bronchial [description not available]	0	3.89	2	0
Eczema, Atopic [description not available]	0	4.86	2	1
Allergic Reaction [description not available]	0	3.89	2	0
Arthritis, Rheumatoid A chronic systemic disease, primarily of the joints, marked by inflammatory changes in the synovial membranes and articular structures, widespread fibrinoid degeneration of the collagen fibers in mesenchymal tissues, and by atrophy and rarefaction of bony structures. Etiology is unknown, but autoimmune mechanisms have been implicated.	0	3.03	1	0
Asthma A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).	1	5.89	2	0
Dermatitis, Atopic A chronic inflammatory genetically determined disease of the skin marked by increased ability to form reagin (IgE), with increased susceptibility to allergic rhinitis and asthma, and hereditary disposition to a lowered threshold for pruritus. It is manifested by lichenification, excoriation, and crusting, mainly on the flexural surfaces of the elbow and knee. In infants it is known as infantile eczema.	1	6.86	2	1
Hypersensitivity Altered reactivity to an antigen, which can result in pathologic reactions upon subsequent exposure to that particular antigen.	0	3.89	2	0

pf-3893787

Description

Cross-References

Synonyms (31)

Protein Targets (6)

Inhibition Measurements

Activation Measurements

Biological Processes (31)

Molecular Functions (15)

Ceullar Components (8)

Bioassays (56)

Research

Studies (6)

Market Indicators

Research Demand Index: 12.43

Study Types

pf-3893787

Description

Cross-References

Synonyms (31)

Protein Targets (6)

Inhibition Measurements

Activation Measurements

Biological Processes (31)

Molecular Functions (15)

Ceullar Components (8)

Bioassays (56)

Research

Studies (6)

Market Indicators

Research Demand Index: 12.43

Study Types

Related Drugs (6)

Related Conditions (8)