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Compound Detail

CHEMBL5819051

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Cc1cc(Cl)cc([C@H](CC(=O)O)NC(=O)CNC(=O)c2cc(O)cc(NC3=NCC(O)CN3)c2)c1

Basic Information

ChEMBL ID CHEMBL5819051
Phase Preclinical
Structure Type MOL
InChI Key UCBYYQWMMNUSGH-IBGZPJMESA-N
10
Targets
14
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

503.9
MW (Da)
1.15
ALogP
8
HBA
7
HBD
172.4
PSA (Ų)
0.28
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26ClN5O6
MW 503.94
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.49

Activity Summary

IC50 14 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-V/beta-5
CHEMBL2096675
IC50 9.4 9.4 0.4 2
Integrin alpha-V/beta-6
CHEMBL2111416
IC50 9.22 9.22 0.6 1
Integrin alpha-5/beta-6
CHEMBL6066570
IC50 9.22 9.22 0.6 1
Integrin alpha-V/beta-8
CHEMBL3430892
IC50 9.15 9.15 0.7 2
Integrin alpha-5/alpha-8
CHEMBL6066569
IC50 9.1 9.1 0.8 1
Integrin alpha-8/beta-1
CHEMBL6066586
IC50 9.1 9.1 0.8 1
Integrin alpha-5/beta-1
CHEMBL2095226
IC50 8.7 8.7 2.0 2
Integrin alpha-V/beta-3
CHEMBL1907598
IC50 8.4 8.4 4.0 2
Integrin alpha-V/beta-1
CHEMBL2111407
IC50 8.4 8.4 4.0 1
Integrin alpha-V/alpha-5
CHEMBL3430893
IC50 8.4 8.4 4.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Integrin alpha-V/beta-5 IC50 = 0.4 nM 9.4 Solid Phase Receptor Assay (SPRA) for alphaVbeta5: Recombinant human vitronectin... -
Integrin alpha-V/beta-5 IC50 = 0.4 nM 9.4 Solid Phase Receptor Assay (SPRA) for alphavbeta5 Function: Recombinant human vi... -
Integrin alpha-V/beta-6 IC50 = 0.6 nM 9.22 Solid Phase Receptor Assay (SPRA) for alphaVbeta6: Recombinant human LAP (R&D Sy... -
Integrin alpha-5/beta-6 IC50 = 0.6 nM 9.22 Solid Phase Receptor Assay (SPRA) for alphavbeta6 Function: Recombinant human LA... -
Integrin alpha-V/beta-8 IC50 = 0.7 nM 9.15 Solid Phase Receptor Assay (SPRA) for alphaVbeta8: Recombinant human LAP protein... -
Integrin alpha-V/beta-8 IC50 = 0.7 nM 9.15 Solid Phase Receptor Assay (SPRA) for alphavbeta8 Function: Recombinant human LA... -
Integrin alpha-8/beta-1 IC50 = 0.8 nM 9.1 Solid Phase Receptor Assay (SPRA) for alpha8beta1: Recombinant mouse nephronecti... -
Integrin alpha-5/alpha-8 IC50 = 0.8 nM 9.1 Solid Phase Receptor Assay (SPRA) for alpha8beta1 Function: Recombinant mouse ne... -
Integrin alpha-5/beta-1 IC50 = 2.0 nM 8.7 Solid Phase Receptor Assay (SPRA) for alpha5beta5: Purified human fibronectin (R... -
Integrin alpha-5/beta-1 IC50 = 2.0 nM 8.7 Solid Phase Receptor Assay (SPRA) for alpha5beta1 Function: Purified human fibro... -
Integrin alpha-V/beta-1 IC50 = 4.0 nM 8.4 Solid Phase Receptor Assay (SPRA) for alphaVbeta1: Purified human fibronectin (R... -
Integrin alpha-V/beta-3 IC50 = 4.0 nM 8.4 Solid Phase Receptor Assay (SPRA) for alphaVbeta3: Recombinant human vitronectin... -
Integrin alpha-V/alpha-5 IC50 = 4.0 nM 8.4 Solid Phase Receptor Assay (SPRA) for alphavbeta1 Function: Purified human fibro... -
Integrin alpha-V/beta-3 IC50 = 4.0 nM 8.4 Solid Phase Receptor Assay (SPRA) for alphavbeta3 Function: Recombinant human vi... -

Data from ChEMBL 36 via Core Engine