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Assay Detail

CHEMBL956592

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

Binding
Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK93 cells
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK93
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Potent benzimidazolone-based CGRP receptor antagonists.
Theberge CR, Bednar RA, Bell IM, Corcoran HA, Fay JF, Hershey JC, Johnston VK, Kane SA, Mosser S, Salvatore CA, Williams TM, Zartman CB, Zhang XF, Graham SL, Vacca JP.
Bioorg Med Chem Lett (2008) 18 : 6122 -6125
PubMed 18947992 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 7.86 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL453643 1 9.29
CHEMBL519421 1 8.77
CHEMBL487068 1 8.72
CHEMBL488082 1 8.68
CHEMBL455458 1 8.66
CHEMBL530116 1 8.57
CHEMBL488083 1 8.37
CHEMBL455674 1 8.33
CHEMBL471358 1 8.26
CHEMBL453644 1 8.15
CHEMBL487244 1 8.02
CHEMBL455670 1 8.02
CHEMBL508016 1 7.89
CHEMBL471530 1 7.89
CHEMBL520905 1 7.82
CHEMBL471706 1 7.82
CHEMBL487076 1 7.75
CHEMBL223156 1 7.68
CHEMBL488255 1 7.68
CHEMBL507339 1 7.66
CHEMBL487077 1 7.64
CHEMBL471704 1 7.58
CHEMBL487240 1 7.58
CHEMBL509718 1 7.51
CHEMBL470321 1 7.50
CHEMBL453865 1 7.44
CHEMBL521076 1 7.43
CHEMBL221009 1 7.42
CHEMBL471359 1 7.39
CHEMBL519242 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL453643 Ki = 0.51 nM 9.29
CHEMBL519421 Ki = 1.7 nM 8.77
CHEMBL487068 Ki = 1.9 nM 8.72
CHEMBL488082 Ki = 2.1 nM 8.68
CHEMBL455458 Ki = 2.2 nM 8.66
CHEMBL530116 Ki = 2.7 nM 8.57
CHEMBL488083 Ki = 4.3 nM 8.37
CHEMBL455674 Ki = 4.7 nM 8.33
CHEMBL471358 Ki = 5.5 nM 8.26
CHEMBL453644 Ki = 7.1 nM 8.15
CHEMBL487244 Ki = 9.5 nM 8.02
CHEMBL455670 Ki = 9.6 nM 8.02
CHEMBL508016 Ki = 13.0 nM 7.89
CHEMBL471530 Ki = 13.0 nM 7.89
CHEMBL471706 Ki = 15.0 nM 7.82
CHEMBL520905 Ki = 15.0 nM 7.82
CHEMBL487076 Ki = 18.0 nM 7.75
CHEMBL223156 Ki = 21.0 nM 7.68
CHEMBL488255 Ki = 21.0 nM 7.68
CHEMBL507339 Ki = 22.0 nM 7.66
CHEMBL487077 Ki = 23.0 nM 7.64
CHEMBL471704 Ki = 26.0 nM 7.58
CHEMBL487240 Ki = 26.0 nM 7.58
CHEMBL509718 Ki = 31.0 nM 7.51
CHEMBL470321 Ki = 32.0 nM 7.50
CHEMBL453865 Ki = 36.0 nM 7.44
CHEMBL521076 Ki = 37.0 nM 7.43
CHEMBL221009 Ki = 38.0 nM 7.42
CHEMBL471359 Ki = 41.0 nM 7.39
CHEMBL519242 Ki = 62.0 nM 7.21
CHEMBL471705 Ki = 100.0 nM 7.00
CHEMBL488065 Ki = 120.0 nM 6.92
CHEMBL488066 Ki = 250.0 nM 6.60