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Assay Detail

CHEMBL973601

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

Binding
Binding affinity to human MC4 receptor
75
Total Activities
75
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Melanocortin receptor 4 (CHEMBL259)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship studies on a series of piperazinebenzylalcohols and their ketone and amine analogs as melanocortin-4 receptor ligands.
Marinkovic D, Tucci FC, Tran JA, Fleck BA, Wen J, Chen C.
Bioorg Med Chem Lett (2008) 18 : 4817 -4822
PubMed 18682322 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 75 7.31 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL487044 1 8.77
CHEMBL365597 1 8.74
CHEMBL505442 1 8.70
CHEMBL487043 1 8.70
CHEMBL511826 1 8.49
CHEMBL488710 1 8.38
CHEMBL488030 1 8.33
CHEMBL462380 1 8.20
CHEMBL528108 1 8.11
CHEMBL513404 1 8.09
CHEMBL471340 1 8.08
CHEMBL454906 1 8.05
CHEMBL454900 1 8.03
CHEMBL454916 1 8.02
CHEMBL454663 1 7.96
CHEMBL508285 1 7.96
CHEMBL366706 1 7.96
CHEMBL471339 1 7.89
CHEMBL508641 1 7.89
CHEMBL462346 1 7.82
CHEMBL512496 1 7.80
CHEMBL454901 1 7.75
CHEMBL471167 1 7.68
CHEMBL462345 1 7.68
CHEMBL447298 1 7.64
CHEMBL460942 1 7.62
CHEMBL528329 1 7.58
CHEMBL514603 1 7.58
CHEMBL454918 1 7.58
CHEMBL509475 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL487044 Ki = 1.7 nM 8.77
CHEMBL365597 Ki = 1.8 nM 8.74
CHEMBL487043 Ki = 2.0 nM 8.70
CHEMBL505442 Ki = 2.0 nM 8.70
CHEMBL511826 Ki = 3.2 nM 8.49
CHEMBL488710 Ki = 4.2 nM 8.38
CHEMBL488030 Ki = 4.7 nM 8.33
CHEMBL462380 Ki = 6.3 nM 8.20
CHEMBL528108 Ki = 7.7 nM 8.11
CHEMBL513404 Ki = 8.1 nM 8.09
CHEMBL471340 Ki = 8.3 nM 8.08
CHEMBL454906 Ki = 9.0 nM 8.05
CHEMBL454900 Ki = 9.4 nM 8.03
CHEMBL454916 Ki = 9.6 nM 8.02
CHEMBL366706 Ki = 11.0 nM 7.96
CHEMBL508285 Ki = 11.0 nM 7.96
CHEMBL454663 Ki = 11.0 nM 7.96
CHEMBL471339 Ki = 13.0 nM 7.89
CHEMBL508641 Ki = 13.0 nM 7.89
CHEMBL462346 Ki = 15.0 nM 7.82
CHEMBL512496 Ki = 16.0 nM 7.80
CHEMBL454901 Ki = 18.0 nM 7.75
CHEMBL471167 Ki = 21.0 nM 7.68
CHEMBL462345 Ki = 21.0 nM 7.68
CHEMBL447298 Ki = 23.0 nM 7.64
CHEMBL460942 Ki = 24.0 nM 7.62
CHEMBL514603 Ki = 26.0 nM 7.58
CHEMBL454918 Ki = 26.0 nM 7.58
CHEMBL528329 Ki = 26.0 nM 7.58
CHEMBL509475 Ki = 28.0 nM 7.55
CHEMBL488884 Ki = 29.0 nM 7.54
CHEMBL471517 Ki = 31.0 nM 7.51
CHEMBL508293 Ki = 32.0 nM 7.50
CHEMBL471516 Ki = 33.0 nM 7.48
CHEMBL452838 Ki = 38.0 nM 7.42
CHEMBL462009 Ki = 42.0 nM 7.38
CHEMBL471166 Ki = 46.0 nM 7.34
CHEMBL529449 Ki = 47.0 nM 7.33
CHEMBL454917 Ki = 49.0 nM 7.31
CHEMBL516659 Ki = 53.0 nM 7.28
CHEMBL519729 Ki = 54.0 nM 7.27
CHEMBL508284 Ki = 65.0 nM 7.19
CHEMBL455189 Ki = 66.0 nM 7.18
CHEMBL455188 Ki = 66.0 nM 7.18
CHEMBL213738 Ki = 74.0 nM 7.13
CHEMBL444749 Ki = 83.0 nM 7.08
CHEMBL462559 Ki = 89.0 nM 7.05
CHEMBL470301 Ki = 91.0 nM 7.04
CHEMBL472553 Ki = 110.0 nM 6.96
CHEMBL458329 Ki = 110.0 nM 6.96