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Compound Detail

CHEMBL4460584

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Cl.Cl.O=C(Nc1ccc(O[C@H]2CCNC2)c(-c2ccc(F)cc2)c1)c1ccc(O[C@H]2CCNC2)c(-c2ccc(F)cc2)c1

Basic Information

ChEMBL ID CHEMBL4460584
Phase Preclinical
Structure Type MOL
InChI Key FIAGMVUVTLWBKV-QLBXQKMFSA-N
Parent Compound CHEMBL4597394
Active Moiety CHEMBL4597394
7
Targets
14
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

555.6
MW (Da)
6.03
ALogP
5
HBA
3
HBD
71.6
PSA (Ų)
0.25
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H33Cl2F2N3O3
MW 628.55
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -0.66

Activity Summary

IC50 9 meas. best 5.15
Ki 5 meas. best 5.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
beta-catenin-B-cell lymphoma 9 protein complex
CHEMBL3885525
Ki 5.18 4.7467 6645.0 3
MDA-MB-231
CHEMBL400
IC50 5.15 5.15 7050.0 1
MDA-MB-435
CHEMBL614697
IC50 5.13 5.13 7397.0 1
beta-catenin-B-cell lymphoma 9 protein complex
CHEMBL3885525
IC50 5.1 4.9767 8017.0 3
HCT-116
CHEMBL394
IC50 5.08 5.08 8231.0 1
SW480
CHEMBL612544
IC50 5.01 5.01 9856.0 1
A549
CHEMBL392
IC50 4.73 4.73 18750.0 1
MCF-10A
CHEMBL614321
IC50 4.7 4.7 19900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
beta-catenin-B-cell lymphoma 9 protein complex Ki = 6645.0 nM 5.18 Inhibition of C-terminal 6x-histidine tagged beta-catenin (138 to 686 residues) ... -
MDA-MB-231 IC50 = 7050.0 nM 5.15 Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability i... -
MDA-MB-435 IC50 = 7397.0 nM 5.13 Cytotoxicity in human MDA-MB-435 cells assessed as reduction in cell viability i... -
beta-catenin-B-cell lymphoma 9 protein complex IC50 = 8017.0 nM 5.1 Inhibition of beta-catenin/BCL9 in Wnt-activated human MDA-MB-231 cells assessed... -
HCT-116 IC50 = 8231.0 nM 5.08 Cytotoxicity in human HCT116 cells assessed as reduction in cell viability incub... -
SW480 IC50 = 9856.0 nM 5.01 Cytotoxicity in human SW480 cells assessed as reduction in cell viability incuba... -
beta-catenin-B-cell lymphoma 9 protein complex IC50 = 9657.0 nM 5.01 Inhibition of beta-catenin/BCL9 in Wnt-activated human SW480 cells assessed as r... -
beta-catenin-B-cell lymphoma 9 protein complex IC50 = 14990.0 nM 4.82 Inhibition of beta-catenin/BCL9 (unknown origin) expressed in Wnt-activated HEK2... -
A549 IC50 = 18750.0 nM 4.73 Cytotoxicity in human A549 cells assessed as reduction in cell viability incubat... -
MCF-10A IC50 = 19900.0 nM 4.7 Cytotoxicity in human MCF10A cells assessed as reduction in cell viability incub... -
beta-catenin-B-cell lymphoma 9 protein complex Ki = 28800.0 nM 4.54 Inhibition of inhibited beta-catenin D145A mutant (unknown origin) expressed in ... -
beta-catenin-B-cell lymphoma 9 protein complex Ki = 30480.0 nM 4.52 Inhibition of inhibited beta-catenin E155A mutant (unknown origin) expressed in ... -

Data from ChEMBL 36 via Core Engine