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Assay Detail

CHEMBL659129

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

Binding
CGRP1 receptor affinity on human neuroblastoma cells SK-N-MC, which selectively express the human CGRP1 receptor.
64
Total Activities
64
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Calcitonin gene-related peptide type 1 receptor (CHEMBL3798)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

From micromolar to nanomolar affinity: a systematic approach to identify the binding site of CGRP at the human calcitonin gene-related peptide 1 receptor.
Rist B, Entzeroth M, Beck-Sickinger AG.
J Med Chem (1998) 41 : 117 -123
PubMed 9438028 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 64 5.44 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL264010 1 7.54
CHEMBL2371143 1 6.84
CHEMBL406459 1 6.80
CHEMBL411804 1 6.77
CHEMBL429765 1 6.70
CHEMBL268539 1 6.69
CHEMBL20034 1 6.66
CHEMBL407854 1 6.55
CHEMBL384581 1 6.52
CHEMBL405511 1 6.44
CHEMBL274851 1 6.33
CHEMBL217867 1 6.31
CHEMBL265906 1 6.21
CHEMBL2371144 1 6.04
CHEMBL216710 1 5.92
CHEMBL407774 1 5.57
CHEMBL440990 1 5.52
CHEMBL407740 1 5.52
CHEMBL407401 1 5.47
CHEMBL404978 1 5.40
CHEMBL269328 1 5.37
CHEMBL262749 1 5.35
CHEMBL406587 1 5.35
CHEMBL411078 1 5.32
CHEMBL216101 1 5.30
CHEMBL386824 1 5.19
CHEMBL415812 1 5.16
CHEMBL428096 1 5.16
CHEMBL265399 1 5.10
CHEMBL275984 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL264010 IC50 = 29.0 nM 7.54
CHEMBL2371143 IC50 = 146.0 nM 6.84
CHEMBL406459 IC50 = 159.0 nM 6.80
CHEMBL411804 IC50 = 170.0 nM 6.77
CHEMBL429765 IC50 = 200.0 nM 6.70
CHEMBL268539 IC50 = 205.0 nM 6.69
CHEMBL20034 IC50 = 220.0 nM 6.66
CHEMBL407854 IC50 = 280.0 nM 6.55
CHEMBL384581 IC50 = 300.0 nM 6.52
CHEMBL405511 IC50 = 360.0 nM 6.44
CHEMBL274851 IC50 = 470.0 nM 6.33
CHEMBL217867 IC50 = 490.0 nM 6.31
CHEMBL265906 IC50 = 620.0 nM 6.21
CHEMBL2371144 IC50 = 910.0 nM 6.04
CHEMBL216710 IC50 = 1200.0 nM 5.92
CHEMBL407774 IC50 = 2700.0 nM 5.57
CHEMBL440990 IC50 = 3000.0 nM 5.52
CHEMBL407740 IC50 = 3000.0 nM 5.52
CHEMBL407401 IC50 = 3400.0 nM 5.47
CHEMBL404978 IC50 = 4000.0 nM 5.40
CHEMBL269328 IC50 = 4275.0 nM 5.37
CHEMBL262749 IC50 = 4500.0 nM 5.35
CHEMBL406587 IC50 = 4500.0 nM 5.35
CHEMBL411078 IC50 = 4790.0 nM 5.32
CHEMBL216101 IC50 = 5000.0 nM 5.30
CHEMBL386824 IC50 = 6500.0 nM 5.19
CHEMBL428096 IC50 = 7000.0 nM 5.16
CHEMBL415812 IC50 = 6900.0 nM 5.16
CHEMBL265399 IC50 = 8000.0 nM 5.10
CHEMBL275984 IC50 = 8550.0 nM 5.07
CHEMBL407697 IC50 = 9000.0 nM 5.05
CHEMBL267137 IC50 = 10000.0 nM 5.00
CHEMBL269027 IC50 = 10000.0 nM 5.00
CHEMBL409205 IC50 = 10000.0 nM 5.00
CHEMBL216229 IC50 = 10000.0 nM 5.00
CHEMBL438224 IC50 = 10000.0 nM 5.00
CHEMBL267182 IC50 = 10000.0 nM 5.00
CHEMBL438008 IC50 = 10000.0 nM 5.00
CHEMBL405694 IC50 = 10000.0 nM 5.00
CHEMBL376040 IC50 = 14000.0 nM 4.85
CHEMBL267406 IC50 = 18000.0 nM 4.75
CHEMBL3350392 IC50 = 19000.0 nM 4.72
CHEMBL404977 IC50 = 24000.0 nM 4.62
CHEMBL439085 IC50 = 24000.0 nM 4.62
CHEMBL405767 IC50 = 32000.0 nM 4.50
CHEMBL262961 IC50 = 45000.0 nM 4.35
CHEMBL410450 IC50 = 51000.0 nM 4.29
CHEMBL266666 IC50 = 70000.0 nM 4.16
CHEMBL410354 IC50 = 80000.0 nM 4.10
CHEMBL269517 IC50 = 95000.0 nM 4.02