Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL47050

PENFLURIDOL
🧪 Phase II
Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
🧪 Phase II
OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1

Basic Information

ChEMBL ID CHEMBL47050
Name PENFLURIDOL
Phase Phase II
Structure Type MOL
InChI Key MDLAAYDRRZXJIF-UHFFFAOYSA-N

Known Names

MCN-JR-16,341 MCN-JR-16341 Micefal NSC-759179 Penfluridol R 16,341 R-16341 Semap
32
Targets
45
Activities
3
Assay Types
0
PK Parameters
20
Publications
8
Known Names
1
Indications

Molecular Properties

524.0
MW (Da)
7.53
ALogP
2
HBA
1
HBD
23.5
PSA (Ų)
0.32
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral
USAN Year 1971

Extended Properties

Molecular Formula C28H27ClF5NO
MW 523.97
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.74

Indications

Psychotic Disorders

ATC Classification

N05AG03
penfluridol
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOLEPTICS

Activity Summary

Ki 25 meas. best 6.9
IC50 19 meas. best 7.21
EC50 1 meas. best 5.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dopamine receptor
CHEMBL2093868
IC50 7.21 7.21 62.0 1
D(1B) dopamine receptor
CHEMBL1850
Ki 6.9 6.9 125.0 1
D(3) dopamine receptor
CHEMBL234
Ki 6.87 6.87 136.0 1
D(1A) dopamine receptor
CHEMBL2056
Ki 6.83 6.83 147.0 1
D(2) dopamine receptor
CHEMBL217
Ki 6.8 6.8 159.0 1
Unchecked
CHEMBL612545
IC50 6.78 5.9386 167.5 7
5-hydroxytryptamine receptor 2B
CHEMBL1833
Ki 6.74 6.74 184.0 1
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 6.55 6.55 280.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 6.45 6.45 356.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.44 6.44 361.0 1
Alpha-2B adrenergic receptor
CHEMBL1942
Ki 6.4 6.4 401.0 1
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 6.35 6.35 445.0 1
Beta-3 adrenergic receptor
CHEMBL246
Ki 6.29 6.29 515.0 1
Sodium-dependent noradrenaline transporter
CHEMBL222
Ki 6.23 6.23 588.0 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 6.22 6.22 602.0 1
Mu-type opioid receptor
CHEMBL233
Ki 6.06 6.06 867.0 1
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 6.05 6.05 881.0 1
5-hydroxytryptamine receptor 5A
CHEMBL3426
Ki 6.0 6.0 1000.0 1
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 6.0 6.0 1000.0 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 6.0 6.0 1000.0 1
Kappa-type opioid receptor
CHEMBL237
Ki 6.0 6.0 1000.0 1
Histamine H1 receptor
CHEMBL231
Ki 6.0 6.0 1000.0 1
D(4) dopamine receptor
CHEMBL219
Ki 6.0 6.0 1000.0 1
Histamine H2 receptor
CHEMBL1941
Ki 6.0 6.0 1000.0 1
Delta-type opioid receptor
CHEMBL236
Ki 5.77 5.77 1714.0 1
Sodium-dependent dopamine transporter
CHEMBL238
Ki 5.77 5.77 1714.0 1
MDA-MB-231
CHEMBL400
IC50 5.64 5.36 2300.0 4
H4
CHEMBL1075452
EC50 5.5 5.5 3200.0 1
5-hydroxytryptamine receptor 1D
CHEMBL1983
Ki 5.45 5.45 3560.0 1
Lewis lung carcinoma cell line
CHEMBL614088
IC50 5.38 5.3233 4200.0 3
SARS-CoV-2
CHEMBL4303835
IC50 5.3 5.3 5010.0 1
NIH3T3
CHEMBL614822
IC50 5.22 5.2167 6010.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dopamine receptor IC50 = 62.0 nM 7.21 Inhibition of [3H]spiroperidol (0.5 nM) binding to dopamine receptor from rat st... 3941416
D(1B) dopamine receptor Ki = 125.0 nM 6.9 Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK293... 30389290
D(3) dopamine receptor Ki = 136.0 nM 6.87 Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed ... 30389290
D(1A) dopamine receptor Ki = 147.0 nM 6.83 Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293... 30389290
D(2) dopamine receptor Ki = 159.0 nM 6.8 Displacement of [3H]N-methylspiperone from human dopamine D2 receptor expressed ... 30389290
Unchecked IC50 = 167.5 nM 6.78 PubChem BioAssay. SNU-C1 viability from Cell TiterGlo-IC50. (Class of assay: c... -
5-hydroxytryptamine receptor 2B Ki = 184.0 nM 6.74 Displacement of [3H]LSD from human 5-HT2B receptor expressed in HEK cells by rad... 30389290
5-hydroxytryptamine receptor 7 Ki = 280.0 nM 6.55 Displacement of [3H]LSD from human 5-HT7A receptor expressed in HEK cells by rad... 30389290
5-hydroxytryptamine receptor 1A Ki = 356.0 nM 6.45 Displacement of [3H]-Way100635 from human 5HT1A receptor expressed in stable CHO... 30389290
5-hydroxytryptamine receptor 2A Ki = 361.0 nM 6.44 Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin) by radiolig... 30389290
Alpha-2B adrenergic receptor Ki = 401.0 nM 6.4 Displacement of [3H]Rauwolscine from human alpha 2B adrenergic receptor expresse... 30389290
Alpha-2C adrenergic receptor Ki = 445.0 nM 6.35 Displacement of [3H]Rauwolscine from human alpha 2C adrenergic receptor expresse... 30389290
Beta-3 adrenergic receptor Ki = 515.0 nM 6.29 Displacement of [3H]CGP12177 from human beta 3 adrenergic receptor expressed in ... 30389290
Sodium-dependent noradrenaline transporter Ki = 588.0 nM 6.23 Displacement of [3H]Nisoxetine from human NET expressed in HEK cells by radiolig... 30389290
Alpha-1D adrenergic receptor Ki = 602.0 nM 6.22 Displacement of [3H]Prazosin from human alpha 1D adrenergic receptor expressed i... 30389290
Mu-type opioid receptor Ki = 867.0 nM 6.06 Displacement of [3H]DAMGO from human MOR expressed in HEK cells by radioligand b... 30389290
5-hydroxytryptamine receptor 2C Ki = 881.0 nM 6.05 Displacement of [3H]Mesulergine from human 5-HT2C receptor expressed in HEK293Fl... 30389290
Unchecked IC50 = 945.9 nM 6.02 PubChem BioAssay. HT-29 viability from Cell TiterGlo-IC50. (Class of assay: co... -
Unchecked IC50 = 961.7 nM 6.02 PubChem BioAssay. Colo320 viability from Cell TiterGlo-IC50. (Class of assay: ... -
Unchecked IC50 = 971.2 nM 6.01 PubChem BioAssay. RKO viability from Cell TiterGlo-IC50. (Class of assay: conf... -

Literature References

PubMed DOI Target Context # Activities
22753 10.1021/jm00199a029 Mus musculus 8
- 10.6019/CHEMBL4651402 SARS-CoV-2 4
3941416 10.1021/jm00151a002 Rattus norvegicus 3
30389290 10.1016/j.bmcl.2018.10.036 Mus musculus 3
30371064 10.1021/acs.jmedchem.8b01044 A549 3
30389290 10.1016/j.bmcl.2018.10.036 MDA-MB-231 3
30389290 10.1016/j.bmcl.2018.10.036 Lewis lung carcinoma cell line 3
30389290 10.1016/j.bmcl.2018.10.036 NIH3T3 3
30371064 10.1021/acs.jmedchem.8b01044 HET-1A 3
30371064 10.1021/acs.jmedchem.8b01044 PC-3 3
30371064 10.1021/acs.jmedchem.8b01044 Caco-2 3
30371064 10.1021/acs.jmedchem.8b01044 ASPC1 3
30389290 10.1016/j.bmcl.2018.10.036 5-hydroxytryptamine receptor 1A 2
30389290 10.1016/j.bmcl.2018.10.036 D(3) dopamine receptor 2
30389290 10.1016/j.bmcl.2018.10.036 D(2) dopamine receptor 2
30389290 10.1016/j.bmcl.2018.10.036 5-hydroxytryptamine receptor 2C 2
30389290 10.1016/j.bmcl.2018.10.036 5-hydroxytryptamine receptor 2B 2
30389290 10.1016/j.bmcl.2018.10.036 5-hydroxytryptamine receptor 2A 2
30389290 10.1016/j.bmcl.2018.10.036 5-hydroxytryptamine receptor 1D 2
30389290 10.1016/j.bmcl.2018.10.036 Mu-type opioid receptor 2

Data from ChEMBL 36 via Core Engine