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Assay Detail

CHEMBL954950

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Functional
Antagonist activity at human CGRP1 receptor in human SK-N-MC cells assessed as effect on human alpha-CGRP-induced cAMP accumulation
ChEMBL ↗
42
Total Activities
34
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SK-N-MC
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Calcitonin gene-related peptide 1 (CHEMBL5293) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.
Miranda LP, Holder JR, Shi L, Bennett B, Aral J, Gegg CV, Wright M, Walker K, Doellgast G, Rogers R, Li H, Valladares V, Salyers K, Johnson E, Wild K.
J Med Chem (2008) 51 : 7889 -7897
PubMed 19053766 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 8.50 9.70
Ki 8 9.17 10.22
EC50 1 10.30 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL525962 — — 1 10.30
CHEMBL503773 — — 2 10.22
CHEMBL509329 — — 2 9.34
CHEMBL525039 — — 2 9.28
CHEMBL524724 — — 1 9.28
CHEMBL503180 — — 1 9.24
CHEMBL525589 — — 1 9.24
CHEMBL509603 — — 2 9.22
CHEMBL525810 — — 2 9.19
CHEMBL500283 — — 1 9.19
CHEMBL510807 — — 1 9.15
CHEMBL2372187 — — 2 9.14
CHEMBL2372188 — — 1 9.07
CHEMBL526728 — — 1 8.99
CHEMBL2372192 — — 1 8.88
CHEMBL526916 — — 1 8.81
CHEMBL509374 — — 1 8.76
CHEMBL507917 — — 1 8.74
CHEMBL524320 — — 1 8.71
CHEMBL504769 — — 1 8.68
CHEMBL525571 — — 2 8.50
CHEMBL2372194 — — 2 8.48
CHEMBL2372193 — — 1 8.46
CHEMBL524361 — — 1 8.45
CHEMBL505912 — — 1 8.42
CHEMBL2372190 — — 1 8.38
CHEMBL525416 — — 1 8.30
CHEMBL501792 — — 1 7.95
CHEMBL2372189 — — 1 7.53
CHEMBL526890 — — 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL525962 — EC50 = 0.05 nM 10.30
CHEMBL503773 — Ki = 0.06 nM 10.22
CHEMBL503773 — IC50 = 0.2 nM 9.70
CHEMBL509329 — Ki = 0.46 nM 9.34
CHEMBL525039 — Ki = 0.53 nM 9.28
CHEMBL524724 — IC50 = 0.53 nM 9.28
CHEMBL503180 — IC50 = 0.57 nM 9.24
CHEMBL525589 — IC50 = 0.58 nM 9.24
CHEMBL509603 — Ki = 0.6 nM 9.22
CHEMBL525810 — Ki = 0.64 nM 9.19
CHEMBL500283 — IC50 = 0.64 nM 9.19
CHEMBL510807 — IC50 = 0.71 nM 9.15
CHEMBL2372187 — Ki = 0.73 nM 9.14
CHEMBL509603 — IC50 = 0.79 nM 9.10
CHEMBL2372188 — IC50 = 0.85 nM 9.07
CHEMBL526728 — IC50 = 1.02 nM 8.99
CHEMBL525039 — IC50 = 1.27 nM 8.90
CHEMBL2372192 — IC50 = 1.31 nM 8.88
CHEMBL526916 — IC50 = 1.56 nM 8.81
CHEMBL509374 — IC50 = 1.74 nM 8.76
CHEMBL509329 — IC50 = 1.73 nM 8.76
CHEMBL507917 — IC50 = 1.82 nM 8.74
CHEMBL524320 — IC50 = 1.97 nM 8.71
CHEMBL504769 — IC50 = 2.1 nM 8.68
CHEMBL525810 — IC50 = 2.18 nM 8.66
CHEMBL2372187 — IC50 = 2.23 nM 8.65
CHEMBL525571 — Ki = 3.19 nM 8.50
CHEMBL2372194 — Ki = 3.3 nM 8.48
CHEMBL2372193 — IC50 = 3.45 nM 8.46
CHEMBL524361 — IC50 = 3.54 nM 8.45
CHEMBL2372194 — IC50 = 3.57 nM 8.45
CHEMBL505912 — IC50 = 3.81 nM 8.42
CHEMBL2372190 — IC50 = 4.15 nM 8.38
CHEMBL525571 — IC50 = 4.87 nM 8.31
CHEMBL525416 — IC50 = 4.98 nM 8.30
CHEMBL501792 — IC50 = 11.21 nM 7.95
CHEMBL2372189 — IC50 = 29.73 nM 7.53
CHEMBL526890 — IC50 = 78.9 nM 7.10
CHEMBL2372191 — IC50 = 79.34 nM 7.10
CHEMBL507637 — IC50 = 89.91 nM 7.05
CHEMBL386763 — IC50 = 740.0 nM 6.13
CHEMBL525237 — IC50 >= 1000.0 nM -