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Assay Detail

CHEMBL718189

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Binding
Binding affinity towards human Melanocortin 3 receptor (hMC3R)
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Melanocortin receptor 3 (CHEMBL4644)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).
Koikov LN, Ebetino FH, Solinsky MG, Cross-Doersen D, Knittel JJ.
Bioorg Med Chem Lett (2003) 13 : 2647 -2650
PubMed 12873485 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 6.73 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441738 AFAMELANOTIDE 4.0 1 9.17
CHEMBL431801 1 7.87
CHEMBL92481 1 7.70
CHEMBL432565 1 7.19
CHEMBL89004 1 7.18
CHEMBL419307 1 6.96
CHEMBL315356 1 6.89
CHEMBL312998 1 6.85
CHEMBL328117 1 6.80
CHEMBL406276 1 6.77
CHEMBL329586 1 6.68
CHEMBL327450 1 6.64
CHEMBL316259 1 6.58
CHEMBL313377 1 6.55
CHEMBL88630 1 6.46
CHEMBL315258 1 6.42
CHEMBL88537 1 6.36
CHEMBL91957 1 6.36
CHEMBL407825 1 6.27
CHEMBL86573 1 6.27
CHEMBL264306 1 6.24
CHEMBL316038 1 6.20
CHEMBL50056 1 6.11
CHEMBL89270 1 6.05
CHEMBL88185 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441738 AFAMELANOTIDE Ki = 0.68 nM 9.17
CHEMBL431801 Ki = 13.5 nM 7.87
CHEMBL92481 Ki = 20.0 nM 7.70
CHEMBL432565 Ki = 65.0 nM 7.19
CHEMBL89004 Ki = 66.5 nM 7.18
CHEMBL419307 Ki = 110.0 nM 6.96
CHEMBL315356 Ki = 130.0 nM 6.89
CHEMBL312998 Ki = 140.0 nM 6.85
CHEMBL328117 Ki = 160.0 nM 6.80
CHEMBL406276 Ki = 170.0 nM 6.77
CHEMBL329586 Ki = 210.0 nM 6.68
CHEMBL327450 Ki = 230.0 nM 6.64
CHEMBL316259 Ki = 260.0 nM 6.58
CHEMBL313377 Ki = 280.0 nM 6.55
CHEMBL88630 Ki = 350.0 nM 6.46
CHEMBL315258 Ki = 380.0 nM 6.42
CHEMBL88537 Ki = 440.0 nM 6.36
CHEMBL91957 Ki = 440.0 nM 6.36
CHEMBL407825 Ki = 540.0 nM 6.27
CHEMBL86573 Ki = 540.0 nM 6.27
CHEMBL264306 Ki = 580.0 nM 6.24
CHEMBL316038 Ki = 630.0 nM 6.20
CHEMBL50056 Ki = 770.0 nM 6.11
CHEMBL89270 Ki = 890.0 nM 6.05
CHEMBL88185 Ki = 1900.0 nM 5.72