Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL925936

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to human MC1bR
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators.
Guo L, Ye Z, Ujjainwalla F, Sings HL, Sebhat IK, Huber J, Weinberg DH, Tang R, MacNeil T, Tamvakopoulos C, Peng Q, MacIntyre E, van der Ploeg LH, Goulet MT, Wyvratt MJ, Nargund RP.
Bioorg Med Chem Lett (2008) 18 : 3242 -3247
PubMed 18479920 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.54 6.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL257759 1 6.51
CHEMBL429854 1 6.16
CHEMBL254589 1 5.87
CHEMBL403420 1 5.18
CHEMBL402769 1 4.79
CHEMBL254757 1 4.70
CHEMBL255286 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL257759 IC50 = 311.6 nM 6.51
CHEMBL429854 IC50 = 695.0 nM 6.16
CHEMBL254589 IC50 = 1339.0 nM 5.87
CHEMBL403420 IC50 = 6586.0 nM 5.18
CHEMBL402769 IC50 = 16370.0 nM 4.79
CHEMBL254757 IC50 = 20000.0 nM 4.70
CHEMBL255286 IC50 = 173500.0 nM -