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Compound Detail

CHEMBL5803148

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Cc1ccc(-n2nccn2)c(C(=O)N2C(C)C3CC(Oc4ccc(C(F)(F)F)cn4)C2C3)n1

Basic Information

ChEMBL ID CHEMBL5803148
Phase Preclinical
Structure Type MOL
InChI Key WXFSUKBBTQWXBQ-UHFFFAOYSA-N
2
Targets
19
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

458.4
MW (Da)
3.46
ALogP
7
HBA
0
HBD
86.0
PSA (Ų)
0.60
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H21F3N6O2
MW 458.44
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.99

Activity Summary

Ki 19 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin/Hypocretin receptor type 1
CHEMBL1075232
Ki 8.3 7.595 5.0 8
Unchecked
CHEMBL612545
Ki 8.3 7.0545 5.0 11

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Orexin/Hypocretin receptor type 1 Ki = 5.0 nM 8.3 Receptor Radioligand Binding Assay: Human Embryonic Kidney 293 cells (HEK293) st... -
Orexin/Hypocretin receptor type 1 Ki = 5.0 nM 8.3 Receptor Radioligand Binding Assay: Human Embryonic Kidney 293 cells (HEK293) st... -
Unchecked Ki = 5.0 nM 8.3 Receptor Radioligand Binding Assay: HEK293 stably expressing human orexin 2 rece... -
Unchecked Ki = 5.0 nM 8.3 Receptor Radioligand Binding Assay: HEK293 stably expressing human orexin 2 rece... -
Unchecked Ki = 6.0 nM 8.22 Receptor Radioligand Binding Assay: HEK293 stably expressing human orexin 2 rece... -
Orexin/Hypocretin receptor type 1 Ki = 8.0 nM 8.1 Receptor Radioligand Binding Assay: Human Embryonic Kidney 293 cells (HEK293) st... -
Orexin/Hypocretin receptor type 1 Ki = 9.0 nM 8.05 Receptor Radioligand Binding Assay: Human Embryonic Kidney 293 cells (HEK293) st... -
Orexin/Hypocretin receptor type 1 Ki = 11.0 nM 7.96 Receptor Radioligand Binding Assay: Human Embryonic Kidney 293 cells (HEK293) st... -
Unchecked Ki = 14.0 nM 7.85 Receptor Radioligand Binding Assay: HEK293 stably expressing human orexin 2 rece... -
Unchecked Ki = 20.0 nM 7.7 Receptor Radioligand Binding Assay: HEK293 stably expressing human orexin 2 rece... -
Orexin/Hypocretin receptor type 1 Ki = 21.0 nM 7.68 Receptor Radioligand Binding Assay: Human Embryonic Kidney 293 cells (HEK293) st... -
Orexin/Hypocretin receptor type 1 Ki = 351.0 nM 6.46 Receptor Radioligand Binding Assay: Human Embryonic Kidney 293 cells (HEK293) st... -
Unchecked Ki = 426.0 nM 6.37 Receptor Radioligand Binding Assay: Human Embryonic Kidney 293 cells (HEK293) st... -
Unchecked Ki = 538.0 nM 6.27 Receptor Radioligand Binding Assay: Human Embryonic Kidney 293 cells (HEK293) st... -
Unchecked Ki = 567.0 nM 6.25 Receptor Radioligand Binding Assay: Human Embryonic Kidney 293 cells (HEK293) st... -
Unchecked Ki = 649.0 nM 6.19 Receptor Radioligand Binding Assay: Human Embryonic Kidney 293 cells (HEK293) st... -
Unchecked Ki = 841.0 nM 6.08 Receptor Radioligand Binding Assay: Human Embryonic Kidney 293 cells (HEK293) st... -
Unchecked Ki = 861.0 nM 6.07 Receptor Radioligand Binding Assay: Human Embryonic Kidney 293 cells (HEK293) st... -
Orexin/Hypocretin receptor type 1 Ki = 1240.0 nM 5.91 Receptor Radioligand Binding Assay: Human Embryonic Kidney 293 cells (HEK293) st... -

Data from ChEMBL 36 via Core Engine