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Assay Detail

CHEMBL1648395

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

Functional
Antagonist activity at recombinant oxytocin receptor expressed in CHO cells assessed as inhibition of vasopressin-induced calcium release after 10 mins by Fluo4-AM staining
17
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Oxytocin receptor (CHEMBL2049)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The characterization of a novel V1b antagonist lead series.
Smethurst CA, Borthwick JA, Gaines S, Watson S, Green A, Schulz MJ, Burton G, Buson AA, Arban R.
Bioorg Med Chem Lett (2011) 21 : 92 -96
PubMed 21146408 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 5.56 8.82
pKi 7 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL582857 NELIVAPTAN 2.0 1 8.82
CHEMBL572709 1 6.50
CHEMBL1643585 1 5.60
CHEMBL1643586 1 5.40
CHEMBL1643584 1 5.30
CHEMBL1643588 1 5.20
CHEMBL1643589 1 5.20
CHEMBL1643590 1 4.70
CHEMBL1643587 1 4.60
CHEMBL1643591 1 4.30
CHEMBL1643592 1 -
CHEMBL1643593 1 -
CHEMBL1643594 1 -
CHEMBL1643595 1 -
CHEMBL1643596 1 -
CHEMBL1643597 1 -
CHEMBL1643598 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL582857 NELIVAPTAN Ki = 1.514 nM 8.82
CHEMBL572709 Ki = 316.23 nM 6.50
CHEMBL1643585 Ki = 2511.89 nM 5.60
CHEMBL1643586 Ki = 3981.07 nM 5.40
CHEMBL1643584 Ki = 5011.87 nM 5.30
CHEMBL1643588 Ki = 6309.57 nM 5.20
CHEMBL1643589 Ki = 6309.57 nM 5.20
CHEMBL1643590 Ki = 19952.62 nM 4.70
CHEMBL1643587 Ki = 25118.86 nM 4.60
CHEMBL1643591 Ki = 50118.72 nM 4.30
CHEMBL1643592 pKi - -
CHEMBL1643593 pKi - -
CHEMBL1643594 pKi - -
CHEMBL1643595 pKi - -
CHEMBL1643596 pKi - -
CHEMBL1643597 pKi - -
CHEMBL1643598 pKi - -