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Compound Detail

CHEMBL5914164

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O=C(O)C[C@H](NC(=O)CNC(=O)c1cncc(NC2=NCC(O)CN2)c1)c1cc(Br)cc(Br)c1

Basic Information

ChEMBL ID CHEMBL5914164
Phase Preclinical
Structure Type MOL
InChI Key SHRSEUHJTZQLRO-KRWDZBQOSA-N
10
Targets
14
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

598.2
MW (Da)
1.40
ALogP
8
HBA
6
HBD
165.0
PSA (Ų)
0.27
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22Br2N6O5
MW 598.25
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.55

Activity Summary

IC50 14 meas. best 10.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Integrin alpha-V/beta-5
CHEMBL2096675
IC50 10.0 10.0 0.1 2
Integrin alpha-V/beta-6
CHEMBL2111416
IC50 9.7 9.7 0.2 1
Integrin alpha-V/beta-8
CHEMBL3430892
IC50 9.7 9.7 0.2 2
Integrin alpha-5/beta-6
CHEMBL6066570
IC50 9.7 9.7 0.2 1
Integrin alpha-V/beta-3
CHEMBL1907598
IC50 9.52 9.52 0.3 2
Integrin alpha-5/alpha-8
CHEMBL6066569
IC50 9.4 9.4 0.4 1
Integrin alpha-8/beta-1
CHEMBL6066586
IC50 9.4 9.4 0.4 1
Integrin alpha-5/beta-1
CHEMBL2095226
IC50 9.22 9.22 0.6 2
Integrin alpha-V/beta-1
CHEMBL2111407
IC50 9.15 9.15 0.7 1
Integrin alpha-V/alpha-5
CHEMBL3430893
IC50 9.15 9.15 0.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Integrin alpha-V/beta-5 IC50 = 0.1 nM 10.0 Solid Phase Receptor Assay (SPRA) for alphaVbeta5: Recombinant human vitronectin... -
Integrin alpha-V/beta-5 IC50 = 0.1 nM 10.0 Solid Phase Receptor Assay (SPRA) for alphavbeta5 Function: Recombinant human vi... -
Integrin alpha-V/beta-6 IC50 = 0.2 nM 9.7 Solid Phase Receptor Assay (SPRA) for alphaVbeta6: Recombinant human LAP (R&D Sy... -
Integrin alpha-V/beta-8 IC50 = 0.2 nM 9.7 Solid Phase Receptor Assay (SPRA) for alphaVbeta8: Recombinant human LAP protein... -
Integrin alpha-5/beta-6 IC50 = 0.2 nM 9.7 Solid Phase Receptor Assay (SPRA) for alphavbeta6 Function: Recombinant human LA... -
Integrin alpha-V/beta-8 IC50 = 0.2 nM 9.7 Solid Phase Receptor Assay (SPRA) for alphavbeta8 Function: Recombinant human LA... -
Integrin alpha-V/beta-3 IC50 = 0.3 nM 9.52 Solid Phase Receptor Assay (SPRA) for alphaVbeta3: Recombinant human vitronectin... -
Integrin alpha-V/beta-3 IC50 = 0.3 nM 9.52 Solid Phase Receptor Assay (SPRA) for alphavbeta3 Function: Recombinant human vi... -
Integrin alpha-8/beta-1 IC50 = 0.4 nM 9.4 Solid Phase Receptor Assay (SPRA) for alpha8beta1: Recombinant mouse nephronecti... -
Integrin alpha-5/alpha-8 IC50 = 0.4 nM 9.4 Solid Phase Receptor Assay (SPRA) for alpha8beta1 Function: Recombinant mouse ne... -
Integrin alpha-5/beta-1 IC50 = 0.6 nM 9.22 Solid Phase Receptor Assay (SPRA) for alpha5beta5: Purified human fibronectin (R... -
Integrin alpha-5/beta-1 IC50 = 0.6 nM 9.22 Solid Phase Receptor Assay (SPRA) for alpha5beta1 Function: Purified human fibro... -
Integrin alpha-V/beta-1 IC50 = 0.7 nM 9.15 Solid Phase Receptor Assay (SPRA) for alphaVbeta1: Purified human fibronectin (R... -
Integrin alpha-V/alpha-5 IC50 = 0.7 nM 9.15 Solid Phase Receptor Assay (SPRA) for alphavbeta1 Function: Purified human fibro... -

Data from ChEMBL 36 via Core Engine