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Compound Detail

CHEMBL3697578

RAZPIPADON
🧪 Phase II
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🧪 Phase II
Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL3697578
Name RAZPIPADON
Phase Phase II
Structure Type MOL
InChI Key ZXIPVZWZRQCIRW-UHFFFAOYSA-N

Known Names

CVL-871 CVL871 Pf-06669571 PF06669571 PW-0464, (-)- Razpipadon
2
Targets
8
Activities
2
Assay Types
0
PK Parameters
4
Publications
6
Known Names
2
Indications

Molecular Properties

389.4
MW (Da)
3.15
ALogP
6
HBA
1
HBD
86.2
PSA (Ų)
0.72
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral
USAN Stem -padon
USAN Year 2023

Extended Properties

Molecular Formula C19H17F2N3O4
MW 389.36
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.29

Indications

Alzheimer Disease Parkinson Disease

Activity Summary

Ki 6 meas. best 8.16
EC50 2 meas. best 8.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(1A) dopamine receptor
CHEMBL2056
 EC50 8.28 8.28 5.3 1
D(1A) dopamine receptor
CHEMBL2056
 Ki 8.16 7.8 6.9 6
D(1B) dopamine receptor
CHEMBL1850
 EC50 7.92 7.92 12.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
D(1A) dopamine receptor EC50 = 5.3 nM 8.28 Agonist activity at wild type human D1R expressed in HEK293 cells assessed as ef... 31098001
D(1A) dopamine receptor Ki = 6.91 nM 8.16 Competition Binding Assay: The affinity of the compounds described herein was de... -
D(1A) dopamine receptor Ki = 6.91 nM 8.16 Receptor Binding Assay: D1 binding assays were performed using over-expressing L... -
D(1B) dopamine receptor EC50 = 12.0 nM 7.92 Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as e... 31098001
D(1A) dopamine receptor Ki = 18.6 nM 7.73 Competition Binding Assay: The affinity of the compounds described herein was de... -
D(1A) dopamine receptor Ki = 18.6 nM 7.73 Human D1 Receptor Binding Assay: The affinity of the compounds described herein ... -
D(1A) dopamine receptor Ki = 18.6 nM 7.73 Receptor Binding Assay: D1 binding assays were performed using over-expressing L... -
D(1A) dopamine receptor Ki = 51.0 nM 7.29 Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell ... 31098001

Literature References

PubMed DOI Target Context # Activities
31098001 10.1021/acsmedchemlett.9b00050 D(1A) dopamine receptor 5
31098001 10.1021/acsmedchemlett.9b00050 D(2) dopamine receptor 2
31098001 10.1021/acsmedchemlett.9b00050 D(4) dopamine receptor 2
31098001 10.1021/acsmedchemlett.9b00050 D(1B) dopamine receptor 2

Data from ChEMBL 36 via Core Engine