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Compound Detail

CHEMBL3883565

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C=CC(=O)NC[C@H](NC(=O)[C@@H](NC(C)=O)[C@@H](C)CC)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@]1(C)CCCC=CCCC[C@@](C)(C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@H]([C@@H](C)CC)NC1=O)[C@@H](C)CC

Basic Information

ChEMBL ID CHEMBL3883565
Phase Preclinical
Structure Type MOL
InChI Key MWULFOCTLISUDK-SLAXOHTASA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

2601.0
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C120H186N34O31
MW 2601.01

Activity Summary

IC50 1 meas. best 8.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bcl-2-related protein A1
CHEMBL6044
IC50 8.07 8.07 8.5 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.4667 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28105269 10.1021/acsmedchemlett.6b00395 Bcl-2-related protein A1 10
28105269 10.1021/acsmedchemlett.6b00395 ADMET 1
28105269 10.1021/acsmedchemlett.6b00395 No relevant target 1
28105269 10.1021/acsmedchemlett.6b00395 Bcl-2-like protein 1 1
28105269 10.1021/acsmedchemlett.6b00395 G1/S-specific cyclin-D1 1
28105269 10.1021/acsmedchemlett.6b00395 Induced myeloid leukemia cell differentiation protein Mcl-1 1

Data from ChEMBL 36 via Core Engine