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Assay Detail

CHEMBL4421025

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Functional
Agonist activity at human amylin receptor expressed in BHK570 cells co-expressing RAMP3 assessed as increase in intracellular cAMP concentration incubated for 3 hrs in presence of 10% FBS by CRE luciferase reporter gene assay
ChEMBL ↗
96
Total Activities
96
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Amylin receptor AMY3; CALCR/RAMP3 (CHEMBL2111190) ↗
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Amylin and calcitonin receptor agonist
(2017)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 96 9.97 10.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4539553 — — 1 10.77
CHEMBL4540998 — — 1 10.72
CHEMBL4559158 — — 1 10.62
CHEMBL4443871 — — 1 10.59
CHEMBL4443487 — — 1 10.59
CHEMBL4514388 — — 1 10.52
CHEMBL4474371 — — 1 10.43
CHEMBL4516363 — — 1 10.42
CHEMBL4538977 — — 1 10.41
CHEMBL4548044 — — 1 10.41
CHEMBL4548390 — — 1 10.36
CHEMBL4436860 — — 1 10.33
CHEMBL4453619 — — 1 10.31
CHEMBL4460698 — — 1 10.29
CHEMBL4535221 — — 1 10.28
CHEMBL4439362 — — 1 10.28
CHEMBL4475282 — — 1 10.24
CHEMBL4439140 — — 1 10.24
CHEMBL4451589 — — 1 10.21
CHEMBL4557587 — — 1 10.21
CHEMBL4451821 — — 1 10.21
CHEMBL4472810 — — 1 10.19
CHEMBL4469128 — — 1 10.19
CHEMBL4521465 — — 1 10.18
CHEMBL4475352 — — 1 10.18
CHEMBL4443697 — — 1 10.17
CHEMBL4453717 — — 1 10.17
CHEMBL4446788 — — 1 10.17
CHEMBL4519563 — — 1 10.17
CHEMBL4585550 — — 1 10.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4539553 — EC50 = 0.017 nM 10.77
CHEMBL4540998 — EC50 = 0.019 nM 10.72
CHEMBL4559158 — EC50 = 0.024 nM 10.62
CHEMBL4443871 — EC50 = 0.026 nM 10.59
CHEMBL4443487 — EC50 = 0.026 nM 10.59
CHEMBL4514388 — EC50 = 0.03 nM 10.52
CHEMBL4474371 — EC50 = 0.037 nM 10.43
CHEMBL4516363 — EC50 = 0.038 nM 10.42
CHEMBL4538977 — EC50 = 0.039 nM 10.41
CHEMBL4548044 — EC50 = 0.039 nM 10.41
CHEMBL4548390 — EC50 = 0.044 nM 10.36
CHEMBL4436860 — EC50 = 0.047 nM 10.33
CHEMBL4453619 — EC50 = 0.049 nM 10.31
CHEMBL4460698 — EC50 = 0.051 nM 10.29
CHEMBL4439362 — EC50 = 0.052 nM 10.28
CHEMBL4535221 — EC50 = 0.052 nM 10.28
CHEMBL4475282 — EC50 = 0.058 nM 10.24
CHEMBL4439140 — EC50 = 0.057 nM 10.24
CHEMBL4451589 — EC50 = 0.061 nM 10.21
CHEMBL4557587 — EC50 = 0.062 nM 10.21
CHEMBL4451821 — EC50 = 0.062 nM 10.21
CHEMBL4472810 — EC50 = 0.064 nM 10.19
CHEMBL4469128 — EC50 = 0.064 nM 10.19
CHEMBL4521465 — EC50 = 0.066 nM 10.18
CHEMBL4475352 — EC50 = 0.066 nM 10.18
CHEMBL4443697 — EC50 = 0.067 nM 10.17
CHEMBL4519563 — EC50 = 0.068 nM 10.17
CHEMBL4453717 — EC50 = 0.067 nM 10.17
CHEMBL4446788 — EC50 = 0.067 nM 10.17
CHEMBL4585550 — EC50 = 0.07 nM 10.15
CHEMBL4452007 — EC50 = 0.071 nM 10.15
CHEMBL4570633 — EC50 = 0.073 nM 10.14
CHEMBL4438518 — EC50 = 0.072 nM 10.14
CHEMBL4466125 — EC50 = 0.074 nM 10.13
CHEMBL4476858 — EC50 = 0.077 nM 10.11
CHEMBL4580205 — EC50 = 0.08 nM 10.10
CHEMBL4463679 — EC50 = 0.081 nM 10.09
CHEMBL4471035 — EC50 = 0.082 nM 10.09
CHEMBL4444482 — EC50 = 0.086 nM 10.07
CHEMBL4443150 — EC50 = 0.085 nM 10.07
CHEMBL4544971 — EC50 = 0.092 nM 10.04
CHEMBL4576946 — EC50 = 0.093 nM 10.03
CHEMBL4476595 — EC50 = 0.094 nM 10.03
CHEMBL4540155 — EC50 = 0.094 nM 10.03
CHEMBL4470867 — EC50 = 0.093 nM 10.03
CHEMBL4584790 — EC50 = 0.1 nM 10.00
CHEMBL4572775 — EC50 = 0.1 nM 10.00
CHEMBL4459158 — EC50 = 0.105 nM 9.98
CHEMBL4473161 — EC50 = 0.106 nM 9.97
CHEMBL4575271 — EC50 = 0.122 nM 9.91