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Assay Detail

CHEMBL908626

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

Binding
Displacement of [125I]CGRP from human recombinant CGRP receptor
51
Total Activities
51
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: optimization of the 4-substituted piperidine.
Burgey CS, Stump CA, Nguyen DN, Deng JZ, Quigley AG, Norton BR, Bell IM, Mosser SD, Salvatore CA, Rutledge RZ, Kane SA, Koblan KS, Vacca JP, Graham SL, Williams TM.
Bioorg Med Chem Lett (2006) 16 : 5052 -5056
PubMed 16889959 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 50 6.49 8.96
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL385454 1 8.96
CHEMBL215325 1 8.20
CHEMBL214507 1 7.96
CHEMBL215274 1 7.96
CHEMBL215499 1 7.96
CHEMBL386757 1 7.72
CHEMBL408093 1 7.64
CHEMBL384799 1 7.58
CHEMBL384539 1 7.57
CHEMBL383872 1 7.57
CHEMBL213976 1 7.54
CHEMBL424864 1 7.32
CHEMBL379548 1 7.29
CHEMBL437718 1 6.98
CHEMBL384408 1 6.96
CHEMBL386204 1 6.84
CHEMBL211931 1 6.81
CHEMBL214800 1 6.69
CHEMBL405544 1 6.58
CHEMBL212942 1 6.53
CHEMBL377252 1 6.50
CHEMBL214904 1 6.47
CHEMBL427743 1 6.46
CHEMBL214873 1 6.43
CHEMBL386113 1 6.37
CHEMBL214845 1 6.24
CHEMBL213670 1 6.23
CHEMBL415453 1 6.16
CHEMBL214829 1 6.14
CHEMBL405543 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL385454 Ki = 1.1 nM 8.96
CHEMBL215325 Ki = 6.3 nM 8.20
CHEMBL215274 Ki = 11.0 nM 7.96
CHEMBL215499 Ki = 11.0 nM 7.96
CHEMBL214507 Ki = 11.0 nM 7.96
CHEMBL386757 Ki = 19.0 nM 7.72
CHEMBL408093 Ki = 23.0 nM 7.64
CHEMBL384799 Ki = 26.0 nM 7.58
CHEMBL384539 Ki = 27.0 nM 7.57
CHEMBL383872 Ki = 27.0 nM 7.57
CHEMBL213976 Ki = 29.0 nM 7.54
CHEMBL424864 Ki = 48.0 nM 7.32
CHEMBL379548 Ki = 51.0 nM 7.29
CHEMBL437718 Ki = 104.0 nM 6.98
CHEMBL384408 Ki = 110.0 nM 6.96
CHEMBL386204 Ki = 143.0 nM 6.84
CHEMBL211931 Ki = 156.0 nM 6.81
CHEMBL214800 Ki = 205.0 nM 6.69
CHEMBL405544 Ki = 260.0 nM 6.58
CHEMBL212942 Ki = 295.0 nM 6.53
CHEMBL377252 Ki = 320.0 nM 6.50
CHEMBL214904 Ki = 339.0 nM 6.47
CHEMBL427743 Ki = 350.0 nM 6.46
CHEMBL214873 Ki = 375.0 nM 6.43
CHEMBL386113 Ki = 427.0 nM 6.37
CHEMBL214845 Ki = 575.0 nM 6.24
CHEMBL213670 Ki = 583.0 nM 6.23
CHEMBL415453 Ki = 685.0 nM 6.16
CHEMBL214829 Ki = 720.0 nM 6.14
CHEMBL405543 Ki = 810.0 nM 6.09
CHEMBL384723 Ki = 853.0 nM 6.07
CHEMBL425807 Ki = 855.0 nM 6.07
CHEMBL215424 Ki = 965.0 nM 6.01
CHEMBL426142 Ki = 983.0 nM 6.01
CHEMBL214950 Ki = 1000.0 nM 6.00
CHEMBL443577 Ki = 1050.0 nM 5.98
CHEMBL386714 Ki = 1055.0 nM 5.98
CHEMBL386701 Ki = 1125.0 nM 5.95
CHEMBL384409 Ki = 2000.0 nM 5.70
CHEMBL381798 Ki = 2250.0 nM 5.65
CHEMBL386706 Ki = 2800.0 nM 5.55
CHEMBL384091 Ki = 2900.0 nM 5.54
CHEMBL375872 Ki = 3800.0 nM 5.42
CHEMBL385399 Ki = 5337.0 nM 5.27
CHEMBL214751 Ki = 6100.0 nM 5.21
CHEMBL384565 Ki = 6400.0 nM 5.19
CHEMBL384080 Ki = 6900.0 nM 5.16
CHEMBL215549 Ki = 20000.0 nM 4.70
CHEMBL213717 Ki = 20000.0 nM 4.70
CHEMBL384772 Activity - -