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Assay Detail

CHEMBL4156525

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Functional
Agonist activity at human RXFP1 expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL ↗
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Relaxin receptor 1 (CHEMBL1293316) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of the first small-molecule relaxin/insulin-like family peptide receptor (RXFP1) agonists: Activation results in an antifibrotic gene expression profile.
Wilson KJ, Xiao J, Chen CZ, Huang Z, Agoulnik IU, Ferrer M, Southall N, Hu X, Zheng W, Xu X, Wang A, Myhr C, Barnaeva E, George ER, Agoulnik AI, Marugan JJ.
Eur J Med Chem (2018) 156 : 79 -92
PubMed 30006176 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 57 5.63 7.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL52606 COLFORSIN 2.0 1 7.33
CHEMBL3715081 — — 1 7.33
CHEMBL3715235 — — 1 7.28
CHEMBL3718400 — — 1 7.17
CHEMBL3716980 — — 1 7.03
CHEMBL3717211 — — 1 6.73
CHEMBL3717389 — — 1 6.73
CHEMBL3717089 — — 1 6.58
CHEMBL3717553 — — 1 6.48
CHEMBL3718541 — — 1 6.33
CHEMBL3715743 — — 1 6.13
CHEMBL3716540 — — 1 6.13
CHEMBL3716462 — — 1 5.97
CHEMBL3717178 — — 1 5.93
CHEMBL3716450 — — 1 5.88
CHEMBL3715203 — — 1 5.78
CHEMBL3716394 — — 1 5.73
CHEMBL1479446 — — 1 5.73
CHEMBL3717723 — — 1 5.73
CHEMBL3719257 — — 1 5.68
CHEMBL4163593 — — 1 5.63
CHEMBL3719295 — — 1 5.63
CHEMBL3718273 — — 1 5.58
CHEMBL3716871 — — 1 5.58
CHEMBL3716596 — — 1 5.58
CHEMBL3716512 — — 1 5.53
CHEMBL3715105 — — 1 5.53
CHEMBL3715551 — — 1 5.48
CHEMBL4162685 — — 1 5.43
CHEMBL3715097 — — 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL52606 COLFORSIN EC50 = 47.0 nM 7.33
CHEMBL3715081 — EC50 = 47.0 nM 7.33
CHEMBL3715235 — EC50 = 52.0 nM 7.28
CHEMBL3718400 — EC50 = 67.0 nM 7.17
CHEMBL3716980 — EC50 = 94.0 nM 7.03
CHEMBL3717211 — EC50 = 188.0 nM 6.73
CHEMBL3717389 — EC50 = 188.0 nM 6.73
CHEMBL3717089 — EC50 = 265.0 nM 6.58
CHEMBL3717553 — EC50 = 334.0 nM 6.48
CHEMBL3718541 — EC50 = 471.0 nM 6.33
CHEMBL3715743 — EC50 = 747.0 nM 6.13
CHEMBL3716540 — EC50 = 747.0 nM 6.13
CHEMBL3716462 — EC50 = 1060.0 nM 5.97
CHEMBL3717178 — EC50 = 1180.0 nM 5.93
CHEMBL3716450 — EC50 = 1320.0 nM 5.88
CHEMBL3715203 — EC50 = 1670.0 nM 5.78
CHEMBL3716394 — EC50 = 1880.0 nM 5.73
CHEMBL1479446 — EC50 = 1880.0 nM 5.73
CHEMBL3717723 — EC50 = 1880.0 nM 5.73
CHEMBL3719257 — EC50 = 2110.0 nM 5.68
CHEMBL4163593 — EC50 = 2360.0 nM 5.63
CHEMBL3719295 — EC50 = 2360.0 nM 5.63
CHEMBL3718273 — EC50 = 2660.0 nM 5.58
CHEMBL3716871 — EC50 = 2650.0 nM 5.58
CHEMBL3716596 — EC50 = 2650.0 nM 5.58
CHEMBL3716512 — EC50 = 2970.0 nM 5.53
CHEMBL3715105 — EC50 = 2970.0 nM 5.53
CHEMBL3715551 — EC50 = 3340.0 nM 5.48
CHEMBL4162685 — EC50 = 3740.0 nM 5.43
CHEMBL3715097 — EC50 = 3740.0 nM 5.43
CHEMBL3717045 — EC50 = 4200.0 nM 5.38
CHEMBL3715539 — EC50 = 4710.0 nM 5.33
CHEMBL3716813 — EC50 = 5290.0 nM 5.28
CHEMBL3716488 — EC50 = 5290.0 nM 5.28
CHEMBL3716127 — EC50 = 5290.0 nM 5.28
CHEMBL3718178 — EC50 = 5930.0 nM 5.23
CHEMBL3718612 — EC50 = 5930.0 nM 5.23
CHEMBL3716581 — EC50 = 7470.0 nM 5.13
CHEMBL3718643 — EC50 = 8380.0 nM 5.08
CHEMBL3715001 — EC50 = 8380.0 nM 5.08
CHEMBL3717718 — EC50 = 9400.0 nM 5.03
CHEMBL3718813 — EC50 = 9400.0 nM 5.03
CHEMBL3718363 — EC50 = 13300.0 nM 4.88
CHEMBL3718895 — EC50 = 29700.0 nM 4.53
CHEMBL3716878 — EC50 = 37400.0 nM 4.43
CHEMBL3715535 — EC50 = 37400.0 nM 4.43
CHEMBL3715266 — EC50 = 59300.0 nM 4.23
CHEMBL3717485 — EC50 = 94000.0 nM 4.03
CHEMBL1491180 — EC50 = 94000.0 nM 4.03
CHEMBL3716714 — EC50 - — -