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Compound Detail

CHEMBL4650365

CAMIZESTRANT
🧪 Phase III
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🧪 Phase III
C[C@@H]1Cc2c(ccc3[nH]ncc23)[C@@H](c2ccc(NC3CN(CCCF)C3)cn2)N1CC(F)(F)F
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL4650365
Name CAMIZESTRANT
Phase Phase III
Structure Type MOL
InChI Key WDHOIABIERMLGY-CMJOXMDJSA-N

Known Names

AZ-14066724 AZ14066724 AZD-9833 Azd9833 Camizestrant
6
Targets
26
Activities
1
Assay Types
14
PK Parameters
16
Publications
5
Known Names
3
Indications
1
Mechanisms

Molecular Properties

476.5
MW (Da)
4.31
ALogP
5
HBA
2
HBD
60.1
PSA (Ų)
0.50
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer
USAN Stem -estr-; -estrant
USAN Year 2021

Extended Properties

Molecular Formula C24H28F4N6
MW 476.52
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.27

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Estrogen receptor alpha degrader DEGRADER Estrogen receptor ✓ ✓

Indications

Breast Neoplasms Breast Neoplasms Liver Diseases

Activity Summary

IC50 26 meas. best 9.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Estrogen receptor
CHEMBL206
 IC50 9.92 8.6025 0.1 16
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
 IC50 8.82 7.904 1.5 5
MCF7
CHEMBL387
 IC50 8.3 7.95 5.0 2
Histamine H3 receptor
CHEMBL264
 IC50 6.48 6.48 330.0 1
Cytochrome P450 3A4
CHEMBL340
 IC50 5.66 5.66 2200.0 1
Cytochrome P450 2D6
CHEMBL289
 IC50 5.37 5.37 4300.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 106.0 % Rattus norvegicus
CL 66.0 % Mus musculus
CL 59.0 mL.min-1.kg-1 Mus musculus
CL 73.0 mL.min-1.kg-1 Rattus norvegicus
CL 12.0 mL.min-1.g-1 Homo sapiens
F 16.0 % Mus musculus
F 19.0 % Rattus norvegicus
Fu 0.15 - Canis lupus familiaris
Fu 0.23 - Mus musculus
Fu 0.26 - Rattus norvegicus
Fu 0.23 - Homo sapiens
Fu 0.23 - Homo sapiens
T1/2 5.1 hr Mus musculus
T1/2 3.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Estrogen receptor IC50 = 0.12 nM 9.92 MCF-7 ER Down-Regulation Assay: The ability of compounds to down-regulate Estrog... -
Estrogen receptor IC50 = 0.1259 nM 9.9 Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERa... 32910656
Estrogen receptor IC50 = 0.1585 nM 9.8 Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERa... 32910656
Estrogen receptor IC50 = 0.1585 nM 9.8 Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ER-... 32910656
Estrogen receptor IC50 = 0.1585 nM 9.8 Induction of ERalpha degradation in human MCF7 cells incubated for 18 to 22 hrs ... 33335676
Estrogen receptor IC50 = 0.17 nM 9.77 MCF-7 ER Down-Regulation Assay: The ability of compounds to down-regulate Estrog... -
Estrogen receptor IC50 = 1.5 nM 8.82 ERalpha Binding Assay: The assay principle is that ER alpha-LBD (GST) is added t... -
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 1.5 nM 8.82 Binding Assay : hERG (human ether go go-related gene) potassium channels are ess... -
Estrogen receptor IC50 = 1.5 nM 8.82 Binding Assay: The assay was performed as follows with all reagent additions car... -
Estrogen receptor IC50 = 1.8 nM 8.74 ERalpha Binding Assay: The assay principle is that ER alpha-LBD (GST) is added t... -
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 1.8 nM 8.74 Binding Assay : hERG (human ether go go-related gene) potassium channels are ess... -
Estrogen receptor IC50 = 1.8 nM 8.74 Binding Assay: The assay was performed as follows with all reagent additions car... -
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 2.1 nM 8.68 Binding Assay : hERG (human ether go go-related gene) potassium channels are ess... -
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 2.4 nM 8.62 Binding Assay : hERG (human ether go go-related gene) potassium channels are ess... -
Estrogen receptor IC50 = 2.4 nM 8.62 Binding Assay: The assay was performed as follows with all reagent additions car... -
Estrogen receptor IC50 = 2.512 nM 8.6 Displacement of fluormone ES2 green reagent from human GST-tagged ERalpha LBD (2... 32910656
Estrogen receptor IC50 = 2.512 nM 8.6 Displacement of fluorescent labelled fluormone ES2 from human recombinant GST ta... 33335676
MCF7 IC50 = 5.012 nM 8.3 Antiproliferative activity against human wild-type MCF7 cells assessed as decrea... 32910656
Estrogen receptor IC50 = 6.31 nM 8.2 Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERa... 32910656
MCF7 IC50 = 25.12 nM 7.6 Antiproliferative activity against human MCF7 cells harboring Y537S mutant asses... 32910656

Literature References

PubMed DOI Target Context # Activities
32910656 10.1021/acs.jmedchem.0c01163 ADMET 21
32910656 10.1021/acs.jmedchem.0c01163 Estrogen receptor 17
32910656 10.1021/acs.jmedchem.0c01163 Unchecked 14
32910656 10.1021/acs.jmedchem.0c01163 No relevant target 12
33335676 10.1021/acsmedchemlett.0c00505 Estrogen receptor 5
33335676 10.1021/acsmedchemlett.0c00505 ADMET 5
32910656 10.1021/acs.jmedchem.0c01163 MCF7 2
32910656 10.1021/acs.jmedchem.0c01163 Cytochrome P450 2C9 1
32910656 10.1021/acs.jmedchem.0c01163 Cytochrome P450 2C19 1
32910656 10.1021/acs.jmedchem.0c01163 Cytochrome P450 1A2 1
32910656 10.1021/acs.jmedchem.0c01163 Histamine H3 receptor 1
32910656 10.1021/acs.jmedchem.0c01163 Voltage-gated inwardly rectifying potassium channel KCNH2 1
32910656 10.1021/acs.jmedchem.0c01163 Cytochrome P450 3A4 1
32910656 10.1021/acs.jmedchem.0c01163 Cytochrome P450 2D6 1
33335676 10.1021/acsmedchemlett.0c00505 No relevant target 1
37377342 10.1021/acs.jmedchem.3c00136 Estrogen receptor 1

Data from ChEMBL 36 via Core Engine