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Assay Detail

CHEMBL2350290

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Functional
Agonist activity at NK3R (unknown origin) transfected in CHO cells assessed as calcium influx at 10 mM
ChEMBL ↗
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neuromedin-K receptor (CHEMBL4429) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists.
Misu R, Noguchi T, Ohno H, Oishi S, Fujii N.
Bioorg Med Chem (2013) 21 : 2413 -2417
PubMed 23473945 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 38 9.95 10.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2347491 — — 1 10.92
CHEMBL583102 — — 1 10.89
CHEMBL2347513 — — 1 10.77
CHEMBL2347510 — — 1 10.62
CHEMBL2347512 — — 1 10.59
CHEMBL2347496 — — 1 10.49
CHEMBL2347498 — — 1 10.44
CHEMBL2347492 — — 1 10.44
CHEMBL2347508 — — 1 10.42
CHEMBL2347494 — — 1 10.40
CHEMBL2347509 — — 1 10.40
CHEMBL2347497 — — 1 10.39
CHEMBL2347493 — — 1 10.37
CHEMBL2347495 — — 1 10.34
CHEMBL2347489 — — 1 10.29
CHEMBL2370235 — — 1 10.22
CHEMBL2347488 — — 1 10.19
CHEMBL2347506 — — 1 10.15
CHEMBL2347361 — — 1 10.14
CHEMBL2347662 — — 1 10.11
CHEMBL2347511 — — 1 10.10
CHEMBL2347657 — — 1 10.10
CHEMBL2347659 — — 1 10.08
CHEMBL2347499 — — 1 10.07
CHEMBL2347501 — — 1 9.96
CHEMBL2347660 UPEROLEIN — 1 9.92
CHEMBL2347661 — — 1 9.89
CHEMBL2347502 — — 1 9.82
CHEMBL436706 KASSININ — 1 9.68
CHEMBL373569 ELEDOISIN 2.0 1 9.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2347491 — EC50 = 0.012 nM 10.92
CHEMBL583102 — EC50 = 0.013 nM 10.89
CHEMBL2347513 — EC50 = 0.017 nM 10.77
CHEMBL2347510 — EC50 = 0.024 nM 10.62
CHEMBL2347512 — EC50 = 0.026 nM 10.59
CHEMBL2347496 — EC50 = 0.032 nM 10.49
CHEMBL2347498 — EC50 = 0.036 nM 10.44
CHEMBL2347492 — EC50 = 0.036 nM 10.44
CHEMBL2347508 — EC50 = 0.038 nM 10.42
CHEMBL2347494 — EC50 = 0.04 nM 10.40
CHEMBL2347509 — EC50 = 0.04 nM 10.40
CHEMBL2347497 — EC50 = 0.041 nM 10.39
CHEMBL2347493 — EC50 = 0.043 nM 10.37
CHEMBL2347495 — EC50 = 0.046 nM 10.34
CHEMBL2347489 — EC50 = 0.051 nM 10.29
CHEMBL2370235 — EC50 = 0.06 nM 10.22
CHEMBL2347488 — EC50 = 0.065 nM 10.19
CHEMBL2347506 — EC50 = 0.071 nM 10.15
CHEMBL2347361 — EC50 = 0.072 nM 10.14
CHEMBL2347662 — EC50 = 0.078 nM 10.11
CHEMBL2347657 — EC50 = 0.079 nM 10.10
CHEMBL2347511 — EC50 = 0.08 nM 10.10
CHEMBL2347659 — EC50 = 0.083 nM 10.08
CHEMBL2347499 — EC50 = 0.085 nM 10.07
CHEMBL2347501 — EC50 = 0.11 nM 9.96
CHEMBL2347660 UPEROLEIN EC50 = 0.12 nM 9.92
CHEMBL2347661 — EC50 = 0.13 nM 9.89
CHEMBL2347502 — EC50 = 0.15 nM 9.82
CHEMBL436706 KASSININ EC50 = 0.21 nM 9.68
CHEMBL373569 ELEDOISIN EC50 = 0.22 nM 9.66
CHEMBL2347362 — EC50 = 0.28 nM 9.55
CHEMBL2347507 — EC50 = 0.47 nM 9.33
CHEMBL2347658 — EC50 = 1.38 nM 8.86
CHEMBL2370372 PHYSALAEMIN EC50 = 3.36 nM 8.47
CHEMBL2347504 — EC50 = 5.04 nM 8.30
CHEMBL2347503 BUFOKININ EC50 = 10.73 nM 7.97
CHEMBL2347500 SIALOKININ II EC50 = 10.88 nM 7.96
CHEMBL2347505 — EC50 = 0.0054 nM -