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Assay Detail

CHEMBL2344728

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Binding
Binding affinity to CGRP receptor (unknown origin)
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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

The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2.
Han X, Civiello RL, Conway CM, Cook DA, Davis CD, Degnan AP, Jiang XJ, Macci R, Mathias NR, Moench P, Pin SS, Schartman R, Signor LJ, Thalody G, Tora G, Whiterock V, Xu C, Macor JE, Dubowchik GM.
Bioorg Med Chem Lett (2013) 23 : 1870 -1873
PubMed 23402880 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 10.00 10.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2336422 1 10.96
CHEMBL2336424 1 10.92
CHEMBL450668 1 10.89
CHEMBL2336411 1 10.82
CHEMBL2336416 1 10.64
CHEMBL2336418 1 10.49
CHEMBL2336417 1 10.41
CHEMBL2336419 1 10.32
CHEMBL2336415 1 10.26
CHEMBL2336412 1 9.85
CHEMBL2336420 1 9.66
CHEMBL454751 1 9.64
CHEMBL2336413 1 9.55
CHEMBL2336414 1 7.96
CHEMBL2336423 1 7.57
CHEMBL2336421 1 -
CHEMBL454791 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2336422 Ki = 0.011 nM 10.96
CHEMBL2336424 Ki = 0.012 nM 10.92
CHEMBL450668 Ki = 0.013 nM 10.89
CHEMBL2336411 Ki = 0.015 nM 10.82
CHEMBL2336416 Ki = 0.023 nM 10.64
CHEMBL2336418 Ki = 0.032 nM 10.49
CHEMBL2336417 Ki = 0.039 nM 10.41
CHEMBL2336419 Ki = 0.048 nM 10.32
CHEMBL2336415 Ki = 0.055 nM 10.26
CHEMBL2336412 Ki = 0.14 nM 9.85
CHEMBL2336420 Ki = 0.22 nM 9.66
CHEMBL454751 Ki = 0.23 nM 9.64
CHEMBL2336413 Ki = 0.28 nM 9.55
CHEMBL2336414 Ki = 11.0 nM 7.96
CHEMBL2336423 Ki = 27.0 nM 7.57
CHEMBL2336421 Ki = 0.005 nM -
CHEMBL454791 Ki = 0.0073 nM -