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Assay Detail

CHEMBL911962

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

Functional
Inhibition of CGRP-induced cAMP production in E10 cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type E10
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

Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists.
Bell IM, Bednar RA, Fay JF, Gallicchio SN, Hochman JH, McMasters DR, Miller-Stein C, Moore EL, Mosser SD, Pudvah NT, Quigley AG, Salvatore CA, Stump CA, Theberge CR, Wong BK, Zartman CB, Zhang XF, Kane SA, Graham SL, Vacca JP, Williams TM.
Bioorg Med Chem Lett (2006) 16 : 6165 -6169
PubMed 17027263 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.76 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL375533 1 7.62
CHEMBL374064 1 7.41
CHEMBL374251 1 7.30
CHEMBL220146 1 7.30
CHEMBL220715 1 7.27
CHEMBL220101 1 7.21
CHEMBL375224 1 7.19
CHEMBL223756 1 7.19
CHEMBL223156 1 7.11
CHEMBL376292 1 6.96
CHEMBL221009 1 6.92
CHEMBL374666 1 6.75
CHEMBL219782 1 6.46
CHEMBL219721 1 6.37
CHEMBL385322 1 6.28
CHEMBL223805 1 6.16
CHEMBL221160 1 5.85
CHEMBL220336 1 5.54
CHEMBL376263 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL375533 IC50 = 24.0 nM 7.62
CHEMBL374064 IC50 = 39.0 nM 7.41
CHEMBL374251 IC50 = 50.0 nM 7.30
CHEMBL220146 IC50 = 50.0 nM 7.30
CHEMBL220715 IC50 = 54.0 nM 7.27
CHEMBL220101 IC50 = 61.0 nM 7.21
CHEMBL375224 IC50 = 64.0 nM 7.19
CHEMBL223756 IC50 = 64.0 nM 7.19
CHEMBL223156 IC50 = 78.0 nM 7.11
CHEMBL376292 IC50 = 110.0 nM 6.96
CHEMBL221009 IC50 = 120.0 nM 6.92
CHEMBL374666 IC50 = 180.0 nM 6.75
CHEMBL219782 IC50 = 350.0 nM 6.46
CHEMBL219721 IC50 = 430.0 nM 6.37
CHEMBL385322 IC50 = 530.0 nM 6.28
CHEMBL223805 IC50 = 690.0 nM 6.16
CHEMBL221160 IC50 = 1400.0 nM 5.85
CHEMBL220336 IC50 = 2900.0 nM 5.54
CHEMBL376263 IC50 = 3300.0 nM 5.48