Fig. 2. (a) Criteria required for the development of a high-throughput chemistry direct-to-biology workflow. (b) Mass spectrum displaying the non-specific adducts formed between an exemplar protein (BRD4-BD1) and an irradiated (302 nm, 10 min) HTC-PhABit containing unreacted succinimide activated ester 1. (c) Protocol for the in-plate synthesis of a library of high-throughput PhABits (HTC-PhABits). 1073 PhABits were synthesised without purification across 4 × 384-well plates. (d) Success rate of the HTC-PhABit synthetic protocol, omitting the 54 impure amine starting materials and the 39 reactions for which conversion was unable to be calculated. (e) Boxplot for the conversion of the HTC-PhABit reactions grouped by the classification of the amine. Amines were classified according to the following categories: hindered vs. unhindered, secondary vs. primary and linear vs. cyclic.